[go: up one dir, main page]

AR053832A1 - Derivados de pirrolidina 3,4 sustituida para el tratamiento de la hipertension - Google Patents

Derivados de pirrolidina 3,4 sustituida para el tratamiento de la hipertension

Info

Publication number
AR053832A1
AR053832A1 ARP060101103A ARP060101103A AR053832A1 AR 053832 A1 AR053832 A1 AR 053832A1 AR P060101103 A ARP060101103 A AR P060101103A AR P060101103 A ARP060101103 A AR P060101103A AR 053832 A1 AR053832 A1 AR 053832A1
Authority
AR
Argentina
Prior art keywords
unsubstituted
substituted
mono
cyclic
alkyl
Prior art date
Application number
ARP060101103A
Other languages
English (en)
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 AR053832A1 publication Critical patent/AR053832A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/24—Oxygen or sulfur atoms
    • C07D207/26—2-Pyrrolidones
    • C07D207/263—2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms
    • C07D207/27—2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A61K31/341—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/351—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom not condensed with another ring
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/357—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/4035—Isoindoles, e.g. phthalimide
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/423—Oxazoles condensed with carbocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4409—Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 4, e.g. isoniazid, iproniazid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4704—2-Quinolinones, e.g. carbostyril
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5355—Non-condensed oxazines and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • 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
    • A61P9/10—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/08—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
    • C07D207/09—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Neurosurgery (AREA)
  • Urology & Nephrology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Vascular Medicine (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)

Abstract

Se refiere al uso de compuestos de pirrolidina (3,4-di-, 3,3,4-tri-, 3,4,4-tri-, o 3,3,4,4-tetra-)-sustituidos, para la preparacion de una formulacion farmacéutica para el tratamiento de una enfermedad que dependa de la actividad de la renina; al uso de un compuesto de esta clase en el tratamiento de una enfermedad que dependa de la actividad de la renina; a compuestos que son parte de una sub-clase de estos compuestos de pirrolidina sustituida para utilizarse en el diagnostico y en el tratamiento terapéutico de un animal de sangre caliente, en especial para el tratamiento de una enfermedad (= trastorno) que dependa de la actividad de la renina; a compuestos que son parte de una sub-clase de estos compuestos de pirrolidina sustituida; a formulaciones farmacéuticas que comprenden a estos compuestos de pirrolidina sustituida, y/o a un método de tratamiento que comprende administrar estos compuestos de pirrolidina sustituida, a un método para la fabricacion en especial de estos compuestos de pirrolidina sustituida, así como a intermediarios, materiales de partida, y/o pasos parciales para su síntesis. Reivindicacion 1: El uso de un compuesto de la formula (1) en donde: R1 es alquilo insustituido o sustituido, arilo mono- o bi-cíclico insustituido o sustituido, heterociclilo mono- o bi-cíclico insustituido o sustituido, cicloalquilo mono- o bi-cíclico insustituido o sustituido, arilo mono- o bi-cíclico -alquilo insustituido o sustituido, heterociclilo mono- o bi-cíclico-alquilo insustituido o sustituido, cicloalquilo mono- o bi-cíclico-alquilo insustituido o sustituido, alquenilo insustituido o sustituido, alquinilo insustituido o sustituido, o acilo; R2 es alquilo insustituido o sustituido, arilo mono- o bi-cíclico insustituido o sustituido, heterociclilo mono- o bi-cíclico insustituido o sustituido, cicloalquilo mono- o bi-cíclico insustituido o sustituido, arilo mono- o bi-cíclico -alquilo insustituido o sustituido, heterociclilo mono- o bi-cíclico-alquilo insustituido o sustituido, cicloalquilo mono- o bi-cíclico-alquilo insustituido o sustituido, alquenilo insustituido o sustituido, alquinilo insustituido o sustituido, o acilo; R3 es una fraccion seleccionada a partir del grupo de fracciones de las formulas (a) a (g) en donde, en cualquiera de las fracciones de las formulas dadas anteriormente baja (a) a (g), el asterisco (*) muestra un enlace que enlaza a la fraccion R3 respectiva con el resto de la molécula en la formula (1); Ra es alquilo insustituido o sustituido, arilo mono- o bi-cíclico insustituido o sustituido, heterociclilo mono- o bi-cíclico insustituido o sustituido, cicloalquilo mono- o bi-cíclico insustituido o sustituido, arilo mono- o bi-cíclico -alquilo insustituido o sustituido, heterociclilo mono- o bi-cíclico-alquilo insustituido o sustituido, cicloalquilo mono- o bi-cíclico-alquilo insustituido o sustituido, acilo, o H; Rb y Rc se seleccionan independientemente a partir de las fracciones dadas en Ra, con la condicion de que de preferencia no más de uno de Rb y Rc sea acilo; Rb y Rc pueden formar juntos un anillo de 3 a 7 miembros que contenga N, el cual puede estar insustituido o sustituido; Rd es alquilo insustituido o sustituido, arilo mono- o bi-cíclico insustituido o sustituido, heterociclilo mono- o bi-cíclico insustituido o sustituido, cicloalquilo mono- o bi-cíclico insustituido o sustituido, arilo mono- o bi-cíclico -alquilo insustituido o sustituido, heterociclilo mono- o bi-cíclico-alquilo insustituido o sustituido, cicloalquilo mono- o bi-cíclico-alquilo insustituido o sustituido, o acilo, o puede tener uno de estos significados, o puede ser -N(Rb(Rc) si m es 1 o de preferencia 2; Re es H, arilo mono- o bi-cíclico -alquilo insustituido o sustituido, heterociclilo mono- o bi-cíclico-alquilo insustituido o sustituido, cicloalquilo mono- o bi-cíclico-alquilo insustituido o sustituido, o alquilo C1-7 sustituido o de preferencia insustituido; y Rf es alquilo insustituido o sustituido, arilo mono- o bi-cíclico insustituido o sustituido, heterociclilo mono- o bi-cíclico insustituido o sustituido, cicloalquilo mono- o bi-cíclico insustituido o sustituido, arilo mono- o bi- cíclico -alquilo insustituido o sustituido, heterociclilo mono- o bi-cíclico-alquilo insustituido o sustituido, cicloalquilo mono- o bi-cíclico-alquilo insustituido o sustituido; m es 0, 1 o 2; cada uno de R4 y R5 se selecciona, independientemente uno del otro, a partir de H, alquilo insustituido o sustituido, hidroxilo, o hidroxilo esterificado o eterificado; y T es metileno, metileno mono- sustituido por alquilo, o es carbonilo o tio-carbonilo; o una sal farmacéuticamente aceptable del mismo, en la preparacion de una formulacion farmacéutica para el tratamiento de una enfermedad que dependa de la actividad de la renina.
ARP060101103A 2005-03-23 2006-03-21 Derivados de pirrolidina 3,4 sustituida para el tratamiento de la hipertension AR053832A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GBGB0505969.6A GB0505969D0 (en) 2005-03-23 2005-03-23 Organic compounds

Publications (1)

Publication Number Publication Date
AR053832A1 true AR053832A1 (es) 2007-05-23

Family

ID=34531739

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP060101103A AR053832A1 (es) 2005-03-23 2006-03-21 Derivados de pirrolidina 3,4 sustituida para el tratamiento de la hipertension

Country Status (26)

Country Link
US (1) US7807709B2 (es)
EP (1) EP1863477B1 (es)
JP (1) JP5171612B2 (es)
KR (1) KR20070113254A (es)
CN (1) CN101146530B (es)
AR (1) AR053832A1 (es)
AT (1) ATE486597T1 (es)
AU (1) AU2006226554B2 (es)
BR (1) BRPI0609671A2 (es)
CA (1) CA2600063A1 (es)
DE (1) DE602006017980D1 (es)
ES (1) ES2355742T3 (es)
GB (1) GB0505969D0 (es)
GT (1) GT200600089A (es)
IL (1) IL185242A0 (es)
MA (1) MA29379B1 (es)
MX (1) MX2007011694A (es)
NO (1) NO20075365L (es)
PE (1) PE20061325A1 (es)
PL (1) PL1863477T3 (es)
PT (1) PT1863477E (es)
RU (1) RU2419606C2 (es)
TN (1) TNSN07361A1 (es)
TW (1) TW200700061A (es)
WO (1) WO2006100036A1 (es)
ZA (1) ZA200706697B (es)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0514203D0 (en) 2005-07-11 2005-08-17 Novartis Ag Organic compounds
EP2420491B1 (en) 2005-12-30 2013-07-03 Novartis AG 3 , 5-substitued piperidine compounds as renin inhibitors
GB0611696D0 (en) * 2006-06-13 2006-07-26 Novartis Ag Organic compounds
EP2119702A4 (en) 2007-01-31 2010-12-08 Dainippon Sumitomo Pharma Co amide derivative
BRPI0813900A2 (pt) 2007-06-25 2014-12-30 Novartis Ag Derivados de n5-(2-etoxietil)-n3-(2-piridinil)-3,5-piperidinodicarboxa mida para uso como inibidores de renina
WO2011136368A1 (ja) 2010-04-28 2011-11-03 協和発酵キリン株式会社 カチオン性脂質
ES2652454T3 (es) * 2011-03-16 2018-02-02 Shanghai Pharmaceuticals Holding Co., Ltd. Compuesto heterocíclico saturado que contiene nitrógeno
JP2013095755A (ja) 2011-11-02 2013-05-20 Kyowa Hakko Kirin Co Ltd カチオン性脂質
CA2858694A1 (en) 2011-12-12 2013-06-20 Kyowa Hakko Kirin Co., Ltd. Lipid nano particles comprising combination of cationic lipids
CN103420890B (zh) * 2012-05-15 2015-06-24 天津药物研究院 3-吡咯甲酸衍生物及其制备方法和用途
CN104471062A (zh) 2012-07-16 2015-03-25 协和发酵麒麟株式会社 抑制KRAS基因表达的RNAi医药组合物
US10022453B2 (en) 2013-12-23 2018-07-17 Bayer Pharma Aktiengesellschaft Antibody drug conjugates (ADCs) with kinesin spindel protein (KSP)
EP3233127A1 (de) 2014-12-15 2017-10-25 Bayer Pharma Aktiengesellschaft Antikörper-wirkstoff-konjugate (adcs) von ksp-inhibitoren mit aglycosylierten anti-tweakrantikörpern
EP4406606A3 (de) 2015-06-22 2024-10-09 Bayer Pharma Aktiengesellschaft Binder-wirkstoff-konjugate (adcs) und binder-prodrug-konjugate (apdcs) mit enzymatisch spaltbaren g
CN107921145A (zh) 2015-06-23 2018-04-17 拜耳医药股份有限公司 Ksp抑制剂与抗‑tweakr抗体的抗体药物缀合物（adc）
US11001636B2 (en) 2016-06-15 2021-05-11 Bayer Pharma Aktiengesellschaft Specific antibody-drug-conjugates (ADCs) with KSP inhibitors and anti-CD123-antibodies
MX2019007641A (es) 2016-12-21 2019-09-09 Bayer Pharma AG Conjugados de ligando-farmaco (adcs) con grupos escindibles enzimaticamente.
CN110072556B (zh) 2016-12-21 2023-05-02 拜耳制药股份公司 具有ksp抑制剂的特异性抗体药物缀合物(adc)
IL294064A (en) * 2019-12-20 2022-08-01 Arbutus Biopharma Corp Synthetic processes and intermediates
CN111423411B (zh) * 2020-04-02 2021-04-16 南京生命源医药科技有限公司 一种新型肾素抑制剂
WO2024033374A1 (en) 2022-08-11 2024-02-15 Syngenta Crop Protection Ag Novel arylcarboxamide or arylthioamide compounds

Family Cites Families (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SE8101536L (sv) * 1981-03-11 1982-09-12 Astra Laekemedel Ab Bensamid-derivat
EP0242789A3 (en) * 1986-04-25 1990-09-05 Dainippon Pharmaceutical Co., Ltd. Novel quinoline derivates and processes for preparation thereof
SG44510A1 (en) 1991-12-18 1997-12-19 Schering Corp Imidazolyl or imidazoylalkyl substituted with a four or five membered nitrogen containing heterocyclic ring
IL111176A0 (en) 1993-10-07 1994-12-29 Du Pont Merck Pharma Dipeptide boronic acid inhibitors of trypsin-like enzymes and pharmaceutical compositions containing them
AU9206798A (en) 1997-08-28 1999-03-16 Merck & Co., Inc. Pyrrolidine and piperidine modulators of chemokine receptor activity
CA2333554A1 (en) 1998-06-17 1999-12-23 Chu-Baio Xue Cyclic hydroxamic acids as metalloproteinase inhibitors
EP1124822A4 (en) 1998-10-30 2002-04-03 Merck & Co Inc THROMBIN INHIBITORS
AU3386500A (en) 1999-03-02 2000-09-21 Merck & Co., Inc. 3-cyclopropyl and 3-cyclobutyl pyrrolidine modulators of chemokine receptor activity
US6489354B1 (en) 1999-03-02 2002-12-03 Merck & Co., Inc. 3-alkyl substituted pyrrolidine modulators of chemokine receptor activity
WO2000051610A1 (en) 1999-03-02 2000-09-08 Merck & Co., Inc. Pyrrolidine modulators of chemokine receptor activity
US6303593B1 (en) 1999-03-02 2001-10-16 Merck & Co., Inc. 3-thienyl and 3-furanyl pyrrolidine modulators of chemokine receptor activity
CZ20023033A3 (cs) 2000-03-17 2003-01-15 Bristol-Myers Squibb Pharma Company Deriváty cyklických beta-aminokyselin jako inhibitory matrixových metaloproteáz a TNF-alfa
FR2811673B1 (fr) 2000-07-17 2002-09-13 Rhodia Chimie Sa Utilisation de composes insatures comprenant un heterocycle comme stabilisants de polymeres halogenes
EP1326619A2 (en) 2000-10-11 2003-07-16 Merck & Co., Inc. Pyrrolidine modulators of ccr5 chemokine receptor activity
WO2003024899A2 (en) 2001-09-17 2003-03-27 Bristol-Myers Squibb Company CYCLIC HYDROXAMIC ACIDS AS INHIBITORS OF MATRIX METALLOPROTEINASES AND/OR TNF-α CONVERTING ENZYME (TACE)
WO2003031443A1 (en) 2001-10-04 2003-04-17 Morphochem Aktiengesellschaft für kombinatorische Chemie Dual actions antibiotics comprising a oxazoldinone and a quinolone or naphthyridinone moiety
DE60324552D1 (en) 2002-05-20 2008-12-18 Bristol Myers Squibb Co Substituierte cycloalkyl p1' hepatitis c virus inhibitoren
GB0212410D0 (en) 2002-05-29 2002-07-10 Novartis Ag Organic compounds
AU2003259131A1 (en) 2002-07-09 2004-01-23 Bristol-Myers Squibb Company Substituted heterocyclic derivatives useful as antidiabetic and antiobesity agents and method
AU2004293178B8 (en) 2003-11-26 2009-01-08 Novartis Ag Organic compounds
WO2005070870A2 (en) 2004-01-23 2005-08-04 Speedel Experimenta Ag Amino alcohol derivatives and their use as renin inhibitors
WO2005070877A1 (en) 2004-01-23 2005-08-04 Speedel Experimenta Ag Diamino alcohols and their use as renin inhibitors
CA2553840A1 (en) 2004-01-23 2005-08-04 Speedel Experimenta Ag Amino alcohol derivatives and their activity as renin inhibitors
BRPI0508961A (pt) 2004-03-19 2007-08-14 Speedel Experimenta Ag derivados de 5-amino-4-hidróxi-7-(1h-indolmetil)-8-metilnonamida como inibidores de renina para o tratamento de hipertensão
EP1725530A1 (en) 2004-03-19 2006-11-29 Speedel Experimenta AG Organic compounds
CN1273452C (zh) * 2004-06-01 2006-09-06 中国医学科学院医药生物技术研究所 7－（4，4－二甲基－3－氨甲基吡咯烷－1－基）取代的新喹啉羧酸衍生物及其制法
TW200631929A (en) 2004-12-10 2006-09-16 Speedel Experimenta Ag ω -phenyloctanamides
GB0428526D0 (en) 2004-12-30 2005-02-09 Novartis Ag Organic compounds
GB0500784D0 (en) 2005-01-14 2005-02-23 Novartis Ag Organic compounds
EP1856032A1 (en) 2005-03-11 2007-11-21 Speedel Experimenta AG Heterocyclic-substituted alkanamides useful as renin inhibitors

Also Published As

Publication number Publication date
AU2006226554B2 (en) 2010-03-11
RU2007138892A (ru) 2009-04-27
ZA200706697B (en) 2008-10-29
GB0505969D0 (en) 2005-04-27
ATE486597T1 (de) 2010-11-15
RU2419606C2 (ru) 2011-05-27
GT200600089A (es) 2006-11-08
JP2008534457A (ja) 2008-08-28
EP1863477A1 (en) 2007-12-12
EP1863477B1 (en) 2010-11-03
TW200700061A (en) 2007-01-01
TNSN07361A1 (en) 2008-12-31
BRPI0609671A2 (pt) 2010-04-20
NO20075365L (no) 2007-12-27
MA29379B1 (fr) 2008-04-01
IL185242A0 (en) 2008-06-05
ES2355742T3 (es) 2011-03-30
CA2600063A1 (en) 2006-09-28
CN101146530B (zh) 2011-05-18
CN101146530A (zh) 2008-03-19
DE602006017980D1 (de) 2010-12-16
WO2006100036A1 (en) 2006-09-28
PT1863477E (pt) 2011-02-10
PE20061325A1 (es) 2007-01-05
KR20070113254A (ko) 2007-11-28
US7807709B2 (en) 2010-10-05
JP5171612B2 (ja) 2013-03-27
US20080194549A1 (en) 2008-08-14
AU2006226554A1 (en) 2006-09-28
MX2007011694A (es) 2007-11-15
PL1863477T3 (pl) 2011-04-29

Similar Documents

Publication Publication Date Title
AR053832A1 (es) Derivados de pirrolidina 3,4 sustituida para el tratamiento de la hipertension
AR046272A1 (es) Inhibidores de dipeptidil peptidasa iv
AR058073A1 (es) Derivados de imidazol 5-il-pirimidina, procesos de obtencion, composiciones farmaceuticas y usos
AR056541A1 (es) Derivados de fenil -1,2,4-oxidiazolona con grupo fenilo ,procedimiento para su preparacion y su uso como productos farmaceuticos
AR058885A1 (es) Compuestos de piperidina 3,5-sustituidos
AR060220A1 (es) Compuestos heterociclicos de 5 o 6 miembros, composiciones farmaceuticas que los comprenden y su uso en la preparacion de medicamentos para el tratamiento de enfermedades asociadas con la dgat1.
RU2013152132A (ru) Борсодержащие малые молекулы в качестве противовоспалительных средств
AR063331A1 (es) Derivados de biaril eter urea y composiciones farmaceuticas
BRPI0817096A8 (pt) Análogo de tiazolidinodiona e composição farmacêutica que o compreende
AR070127A1 (es) Pirrolo - pirimidinas y pirrolo -piridinas
ECSP12011857A (es) Compuestos de dióxido de iminotiadiazina como inhibidores de bace, composiciones, y su uso
AR064608A1 (es) Derivados de pirazolo-quinazolina sustituidos, composiciones farmaceuticas que los contienen. proceso para su preparacion y uso de los mismos como agentes anticancer.
AR026122A1 (es) Derivados de 3(5)-amino-pirazol, procedimiento para su preparacion y su uso como agente antitumorales
AR072906A1 (es) Nucleosidos modificados utiles como antivirales
AR083849A1 (es) Antagonistas de mdm2 de espiro-oxindol
AR068045A1 (es) Derivados de catecolamina y prodrogas de los mismos
AR044749A1 (es) Inhibidor de la arn polimerasa dependiente de arn del virus de la hepatitis c y composiciones y tratamientos que lo usan
BR0102607A (pt) Compostos de difeniluréia, um processo para sua preparação e composições farmacêuticas contendo os mesmos
AR055017A1 (es) Derivados de amida, un proceso para su preparacion, composicion farmaceutica y uso del compuesto para la fabricacion de farmacos
AR056892A1 (es) Derivados de cinolin-3-carboxamida, metodos para su preparacion, composiciones farmaceuticas que los contienen y su uso en la fabricacion de medicamentos para el tratamiento de enfermedades mediadas por la modulacion del receptor gabaa
AR065583A1 (es) Compuestos macrociclicos y composicion farmaceutica
AR045999A1 (es) Compuesto de eter de piperidina, su uso para la fabricacion de un medicamento, composicion farmaceutica que lo comprende y procedimiento para prepararlo
BRPI0607600A2 (pt) derivados de 4-oxoquinazolin-3-il-benzamida para o tratamento de doenças relacionadas com citocina
AR012436A1 (es) Compuestos de 4-aminopirido[2,3-d]pirimidina 5,7-disustituidos, composicion farmaceutica que los comprende, el uso de los mismos para lamanufactura de medicamentos, un procedimiento para su preparacion.
AR040968A1 (es) Bifenilcarboxamidas sustituidas con n- aril piperidina, un metodo para su preparacion, composicion farmaceutica y proceso de preparacion

Legal Events

Date Code Title Description
FB Suspension of granting procedure