AR097086A1 - Derivados 1,3-disustituidos de ciclopentano - Google Patents

Derivados 1,3-disustituidos de ciclopentano

Info

Publication number
AR097086A1
AR097086A1 ARP140102798A ARP140102798A AR097086A1 AR 097086 A1 AR097086 A1 AR 097086A1 AR P140102798 A ARP140102798 A AR P140102798A AR P140102798 A ARP140102798 A AR P140102798A AR 097086 A1 AR097086 A1 AR 097086A1
Authority
AR
Argentina
Prior art keywords
denotes
atoms
hal
substituted
mono
Prior art date
Application number
ARP140102798A
Other languages
English (en)
Inventor
Dr Tsaklakidis Christos
Dr Staehle Wolfgang
Dr Leuthner Birgitta
Original Assignee
Merck Patent Ges Mit Beschränkter Haftung
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 Merck Patent Ges Mit Beschränkter Haftung filed Critical Merck Patent Ges Mit Beschränkter Haftung
Publication of AR097086A1 publication Critical patent/AR097086A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • C07D233/61—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms not forming part of a nitro radical, attached to ring nitrogen atoms
    • 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
    • A61K31/4164—1,3-Diazoles
    • 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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
    • 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
    • A61K31/4192—1,2,3-Triazoles
    • 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
    • A61K31/4196—1,2,4-Triazoles
    • 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
    • A61K31/41—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
    • A61K31/425—Thiazoles
    • A61K31/428—Thiazoles 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory 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
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • 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
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • 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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • C07D233/60—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms with hydrocarbon radicals, substituted by oxygen or sulfur atoms, attached to ring nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/04—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles
    • C07D249/06—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles with aryl radicals directly attached to ring atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • 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
    • C07D401/14—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 three or more hetero rings
    • 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
    • C07D403/10—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 carbon chain containing aromatic rings
    • 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
    • C07D413/10—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 carbon chain containing aromatic rings
    • 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
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Biomedical Technology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Reproductive Health (AREA)
  • Oncology (AREA)
  • Pulmonology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Thiazole And Isothizaole Compounds (AREA)

Abstract

Son inhibidores de la ácido grasa sintasa y se pueden emplear, inter alia, para el tratamiento de enfermedades tales como cáncer, enfermedades cardiovasculares, lesión del sistema nervioso central y diferentes formas de inflamación. Reivindicación 1: Compuestos de la fórmula (1) en donde R denota Ar o Het; Y denota -CO-W o -N(R⁴)CO-W¹; W denota NR²R², Het¹, CH₂Het¹, A, Cyc, Ar o CH₂Ar, -CONR²R² o Het¹; W¹ denota NR²R², Het¹, CH₂Het¹, A, Cyc, Ar, CH₂Ar, CH₂Cyc o CH(OH)CH₂OH; R¹ denota H, F, Cl, Br, OH, CN, NO₂, A, OA, SA, SO₂Me, COA, CONH₂, CONHA o CONA₂; R², R² denotan cada uno, de modo independiente entre si, H, A o [C(R³)₂]ₙCyc; X¹, X², X³ denotan cada uno, de modo independiente entre sí, CR⁸ o N; X⁴ denota CR⁸ o N; X⁵ denota CR⁸ o N; R⁴ denota H o A; A denota alquilo no ramificado o ramificado con 1 - 10 átomos de C, en donde dos átomos de carbono adyacentes pueden formar un enlace doble y/o uno o dos grupos CH y/o CH₂ no adyacentes pueden estar reemplazados por átomos de N, O y/o S y en donde 1 - 7 átomos de H pueden estar reemplazados por R⁵; Cyc denota cicloalquilo con 3 - 7 átomos de C, que no está sustituido o que está monosustituido con OH, Hal o A; A denota alquilo no ramificado o ramificado con 1 - 6 átomos de C, en donde 1 - 5 átomos de H pueden estar reemplazados por F; R⁵ denota F, Cl u OH; Ar denota fenilo, que no está sustituido o que está mono-, di-, tri-, tetra- o pentasustituido con Hal, A, O[C(R³)₂]ₙHet¹, Ar¹, [C(R³)₂]ₚOR³, [C(R³)₂]ₚN(R³)₂, NO₂, CN, [C(R³)₂]ₚCOOR³, CON(R³)₂, Het¹, OCH₂Cyc, [C(R³)₂]ₚN(R³)₂, N(R³)₂COA, NR³SO₂A, [C(R³)₂]ₚSO₂N(R³)₂, S(O)ₙA, O[C(R³)₂]ₘN(R³)₂, NHCOOA, NHCON(R³)₂ y/o COA; Ar¹ denota fenilo o naftilo, que no está sustituido o que está mono-, di-, tri-, tetra- o pentasustituido con Hal, A, [C(R³)₂]ₚOR³, [C(R³)₂]ₚN(R³)₂, NO₂, CN, [C(R³)₂]ₚCOOR³, [C(R³)₂]ₚN(R³)₂, N(R³)₂COA, NR³SO₂A, [C(R³)₂]ₚSO₂N(R³)₂, S(O)ₙA, O[C(R³)₂]ₘN(R³)₂, NHCOOA, NHCON(R³)₂ y/o COA; R³ denota H o alquilo no ramificado o ramificado con 1 - 6 átomos de C; R⁸ denota H o A; Het denota un heterociclo saturado, insaturado o aromático mono- o bicíclico que tiene 1 a 4 átomos de N, O y/o S, que no está sustituido o que está mono-, di-, tri-, tetra- o pentasustituido con Hal, A, O[C(R³)₂]ₙOA, [C(R³)₂]ₙN(R³)₂, SR³, NO₂, CN, COOR³, CON(R³)₂, COHet¹, NR³COA, NR³SO₂A, SO₂N(R³)₂, S(O)ₙA, O[C(R³)₂]ₘN(R³)₂, NHCOOA, NHCON(R³)₂, CHO, COA, =S, =NH, =NA Y/U =O (oxígeno del carbonilo); Het¹ denota un heterociclo saturado, insaturado o aromático mono- o bicíclico que tiene 1 a 4 átomos de N, O y/o S, que no está sustituido o que está mono-, di-, tri-, tetra- o pentasustituido con Hal, A, [C(R³)₂]ₙOR³, [C(R³)₂]ₙN(R³)₂, SR³, NO₂, CN, COOR³, CON(R³)₂, NR³COA, NR³SO₂A, SO₂N(R³)₂, S(O)ₙA, O[C(R³)₂]ₘN(R³)₂, NHCOOA, NHCON(R³)₂, CHO, COA, =S, =NH, =NA Y/U =O (oxígeno del carbonilo); Hal denota F, Cl, Br o I; m denota 1, 2 ó 3; n denota 0, 1 ó 2; p denota 0, 1, 2, 3 ó 4;q denota 0, 1, 2 ó 3; y sus sales, tautómeros, estereoisómeros farmacéuticamente aceptables, incluyendo sus mezclas en todas las proporciones.
ARP140102798A 2013-07-29 2014-07-28 Derivados 1,3-disustituidos de ciclopentano AR097086A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP13003769 2013-07-29

Publications (1)

Publication Number Publication Date
AR097086A1 true AR097086A1 (es) 2016-02-17

Family

ID=48900740

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP140102798A AR097086A1 (es) 2013-07-29 2014-07-28 Derivados 1,3-disustituidos de ciclopentano

Country Status (14)

Country Link
US (1) US9718785B2 (es)
EP (1) EP3027599B1 (es)
JP (1) JP6417415B2 (es)
KR (1) KR20160037986A (es)
CN (1) CN105392785B (es)
AR (1) AR097086A1 (es)
AU (1) AU2014298959B2 (es)
BR (1) BR112016001978A2 (es)
CA (1) CA2919552C (es)
ES (1) ES2633969T3 (es)
IL (1) IL243733A0 (es)
MX (1) MX2016001134A (es)
SG (1) SG11201600726QA (es)
WO (1) WO2015014446A1 (es)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ME03564B (me) 2013-03-13 2020-07-20 Forma Therapeutics Inc DERIVATI 2-HIDROKSI-1-{4-[(4-FENILFENIL)KARBONIL]PIPERAZIN-1-IL}ETAN-1-ONA l SRODNA JEDINJENJA KAO INHIBITORI SINTAZE MASNIH KISELINA (FASN) ZA LEČENJE KANCERA
JP6999424B2 (ja) 2015-06-18 2022-01-18 エイティナイン バイオ リミテッド １，４－置換ピペリジン誘導体
JP6986972B2 (ja) * 2015-06-18 2021-12-22 エイティナイン バイオ リミテッド 置換４−ベンジル及び４−ベンゾイルピペリジン誘導体
TWI808055B (zh) 2016-05-11 2023-07-11 美商滬亞生物國際有限公司 Hdac 抑制劑與 pd-1 抑制劑之組合治療
TWI794171B (zh) 2016-05-11 2023-03-01 美商滬亞生物國際有限公司 Ｈｄａｃ抑制劑與ｐｄ-ｌ１抑制劑之組合治療
TWI830733B (zh) * 2018-05-11 2024-02-01 中國大陸商迪哲（江蘇）醫藥有限公司 環戊烷化合物
CN109320686B (zh) * 2018-08-29 2021-06-08 华南理工大学 一种聚异脲类聚合物及其制备方法和应用
TWI767148B (zh) 2018-10-10 2022-06-11 美商弗瑪治療公司 抑制脂肪酸合成酶(fasn)
CN113382633A (zh) 2018-10-29 2021-09-10 福马治疗股份有限公司 (4-(2-氟-4-(1-甲基-1H-苯并[d]咪唑-5-基)苯甲酰基)哌嗪-1-基)(1-羟基环丙基)甲酮的固体形式

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1499597A4 (en) * 2002-04-08 2006-01-25 Univ Ohio State Res Found COMPOUNDS AND METHODS FOR INDUCING APOPTOSIS IN PROLIFERATION CELLS
US7683176B2 (en) 2006-07-14 2010-03-23 Chemocentryx, Inc. Triazolyl pyridyl benzenesulfonamides
US7718683B2 (en) 2006-07-14 2010-05-18 Chemocentryx, Inc. Triazolyl phenyl benzenesulfonamides
EP2225229A1 (en) 2007-11-26 2010-09-08 Pfizer Inc. Pyrazole derivatives as 5-lo inhibitors
EP2307377A1 (en) * 2008-06-18 2011-04-13 Pfizer Limited Nicotinamide derivatives
WO2011048018A1 (en) * 2009-10-19 2011-04-28 Boehringer Ingelheim International Gmbh Cyclopentanecarboxamide derivatives, medicaments containing such compounds and their use
US20130196971A1 (en) 2010-09-17 2013-08-01 Christopher Joseph Aquino Fatty acid synthase inhibitors
WO2013028445A1 (en) * 2011-08-19 2013-02-28 Glaxosmithkline Llc Fatty acid synthase inhibitors
WO2014075754A1 (en) * 2012-11-16 2014-05-22 Merck Patent Gmbh 3-aminocyclopentane carboxamide derivatives
JP6377732B2 (ja) * 2013-06-21 2018-08-22 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ １，３−ジアミノシクロペンタンカルボキサミド誘導体
ES2671398T3 (es) * 2013-08-16 2018-06-06 Merck Patent Gmbh Derivados de ciclopentilamina 3-sustituida

Also Published As

Publication number Publication date
EP3027599A1 (en) 2016-06-08
JP2016527256A (ja) 2016-09-08
ES2633969T3 (es) 2017-09-26
CN105392785B (zh) 2017-12-22
JP6417415B2 (ja) 2018-11-07
SG11201600726QA (en) 2016-03-30
US20160176824A1 (en) 2016-06-23
CN105392785A (zh) 2016-03-09
WO2015014446A1 (en) 2015-02-05
MX2016001134A (es) 2016-04-29
EP3027599B1 (en) 2017-04-19
AU2014298959B2 (en) 2018-04-05
KR20160037986A (ko) 2016-04-06
CA2919552C (en) 2022-03-15
US9718785B2 (en) 2017-08-01
CA2919552A1 (en) 2015-02-05
BR112016001978A2 (pt) 2017-08-01
IL243733A0 (en) 2016-04-21
AU2014298959A1 (en) 2016-03-10

Similar Documents

Publication Publication Date Title
AR097086A1 (es) Derivados 1,3-disustituidos de ciclopentano
AR092211A1 (es) Derivados de hidropirrolopirrol
AR096296A1 (es) Derivados de 1,3-diaminociclopentacarboxamida
AR094313A1 (es) Inhibidores de fosfatidilinositol 3-quinasa
AR096235A1 (es) Arilquinazolinas
AR090121A1 (es) Compuestos de oxazolidin-2-ona y usos de los mismos
AR089944A1 (es) Derivados de tetrahidro-quinazolinona
AR091156A1 (es) Nucleosidos de espirooxetano de uracilo
AR100006A1 (es) Derivados de tubulisina
AR106595A1 (es) COMPUESTOS HETEROCÍCLICOS COMO INHIBIDORES DE PI3K-g
AR094314A1 (es) Inhibidores de fosfatidilinositol 3-cinasa
AR095326A1 (es) Heterociclos tricíclicos como inhibidores de la proteína bet
AR092365A1 (es) Derivados de piridopirimidina
AR090590A1 (es) COMPUESTOS 1,3,4-OXADIAZOL Y 1,3,4-TIADIAZOL COMO INHIBIDORES DE b-LACTAMASA
AR089945A1 (es) DERIVADOS DE FURO[3,2-B] Y TIENO[3,2-B]PIRIDINA COMO MODULADORES DE TBK1 E IKKe
BR112013025387A2 (pt) análogos substituídos da n-fenilpirimidin-2-amina como inibidores da quinase axl
AR090602A1 (es) AMIDAS CICLICAS Y HETEROCICLOS COMO INHIBIDORES DE MetAP-2
AR086817A1 (es) Compuestos inhibidores de la fosfodiesterasa tipo 10a
AR106053A1 (es) Compuestos imidazo[4,5-c]quinolin-2-ona y su uso para el tratamiento del cáncer
AR092959A1 (es) Derivados de nucleosidos 2-metil sustituidos y metodos de uso de los mismos para el tratamiento de enfermedades virales
CR11757A (es) Compuestos de triazina como inhibidores mtor y quinasa pi3
AR092670A1 (es) Derivados de quinazolinona
BR112015026023A2 (pt) derivados de 2- aminopirido[4,3-d]pirimidin-5-ona e seu uso como inibidores de wee-1
AR098776A1 (es) Derivados del isocromeno como inhibidores de las fosfoinositido-3 quinasas
CO6491087A2 (es) Compuestos de urea que contienen heteroarilo 5,6 bicíclicos como inhibidores de quinasa

Legal Events

Date Code Title Description
FB Suspension of granting procedure