[go: up one dir, main page]

AR070750A1 - Compuestos b1-antagonistas, sus sales farmaceuticamente compatibles, medicamentos que contienen dichos compuestos, uso de los mismos para preparar medicamentos y procedimientoo de preparacion de un medicamento - Google Patents

Compuestos b1-antagonistas, sus sales farmaceuticamente compatibles, medicamentos que contienen dichos compuestos, uso de los mismos para preparar medicamentos y procedimientoo de preparacion de un medicamento

Info

Publication number
AR070750A1
AR070750A1 ARP080103747A ARP080103747A AR070750A1 AR 070750 A1 AR070750 A1 AR 070750A1 AR P080103747 A ARP080103747 A AR P080103747A AR P080103747 A ARP080103747 A AR P080103747A AR 070750 A1 AR070750 A1 AR 070750A1
Authority
AR
Argentina
Prior art keywords
alkyl
substituted
group
fluorine atoms
cycloalkyl
Prior art date
Application number
ARP080103747A
Other languages
English (en)
Inventor
Angelo Ceci
Ingo Konetzki
Juergen Mack
Henning Priepke
Norbert Hauel
Enzo Cereda
Annette Schuler-Metz
Henri Doods
Walter Rainer
Original Assignee
Boehringer Ingelheim Int
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 Boehringer Ingelheim Int filed Critical Boehringer Ingelheim Int
Publication of AR070750A1 publication Critical patent/AR070750A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/24—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring of the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00—Sulfones; Sulfoxides
    • C07C317/44—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/42—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
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/63—One oxygen atom
    • C07D213/64—One oxygen atom attached in position 2 or 6
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • C07D213/82—Amides; Imides in position 3
    • 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
    • C07D233/90—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
    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three 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
    • C07D237/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/34—One oxygen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/34—One oxygen atom
    • C07D239/36—One oxygen atom as doubly bound oxygen atom or as unsubstituted hydroxy radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
    • C07D261/10—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more 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
    • C07D261/18—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/30—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D263/34—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three 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
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three 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
    • C07D277/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/56—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three 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
    • C07D307/68—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06139—Dipeptides with the first amino acid being heterocyclic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/02—Systems containing only non-condensed rings with a three-membered ring

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Indole Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

Reivindicacion 1: Compuestos caracterizados porque tienen la formula general (1) en la cual R1 es (a) un grupo alquilo C1-6 eventualmente sustituido con un radical R1,1, (b) un grupo alquilo C1-3, en el que cada grupo metileno está sustituido con hasta dos átomos de fluor y cada grupo metilo está sustituido con hasta tres átomos de fluor, (c) un grupo cicloalquilo C3-6 eventualmente sustituido con un radical R1,2, (d) un grupo alquenilo C2-6, (e) un grupo alquinilo C2-6, (f) un grupo aril-alquileno C0-2 eventualmente sustituido con 1, 2 o 3 radicales R1,3, (g) un radical heteroarilo de cinco miembros eventualmente sustituido con 1, 2 o 3 radicales R1,4, que al menos contiene un átomo de N, O o S y que eventualmente contiene además uno, dos o tres otros átomos de N y que además puede estar benzocondensado, (h) un radical heteroarilo de seis miembros eventualmente sustituido con un radical R1,4, que contiene uno, dos o tres átomos de N y que además puede estar benzocondensado, (i) -O-R1,1,1 o (j) -NR1,1,2R1,1,4; R1,1 es halogeno, -NO2, -CN, cicloalquilo C3-6, -OR1,1,1, -SR1,1,1, -C(O)R1,1,1, -S(O)2-R1,1,2, -OS(O)2-R1,1,1, -CO2R1,1,1, -OC(O)-R1,1,1, NR1,1,3R1,1,4, -NR1,1,3-C(O)R1,1,1, -NR1,1,3-C(O)-R1,1,1, -NR1,1,3-C(O)2-R1,1,1 o -C(O)-NR1,1,3R1,1,4; R1,1,1 es (a) H, (b) alquilo C1-4, (c) alquilo C1-3, en el que cada grupo metileno está sustituido con hasta dos átomos de fluor y cada grupo metilo está sustituido con hasta tres átomos de fluor, (d) un grupo fenilo eventualmente sustituido con 1, 2 o 3 radicales R1,1,1,1, (e) cicloalquilo C3-6 o (f) un grupo piridilo eventualmente sustituido con 1, 2 o 3 radicales R1,1,1,2; R1,1,1,1 de modo independiente entre sí, es (a) halogeno, -NO2, -CN, -OH, -O-alquilo C1-4, cicloalquilo C3-6, alquilo C1-4 o (b) alquilo C1-3 en el que cada grupo metileno está sustituido con hasta dos átomos de fluor y cada grupo metilo está sustituido con hasta tres átomos de fluor; R1,1,1,2 de modo independiente entre sí, es halogeno o alquilo C1-4; R1,1,2 es (a) alquilo C1-4, (b) alquilo C1-3, en el que cada grupo metileno está sustituido con hasta dos átomos de fluor y cada grupo metilo está sustituido con hasta tres átomos de fluor, (c) -O-alquilo C1-4 o (d) un grupo fenilo eventualmente sustituido con 1, 2 o 3 radicales R1,1,1,1; R1,1,3, R1,1,4 son, de modo independiente entre sí, (a) H, (b) un grupo alquilo C1-4 eventualmente sustituido con 1, 2 o 3 radicales R1,1,4,1, (c) un grupo fenilo eventualmente sustituido con 1, 2 o 3 radicales R1,1,1,1, (d) cicloalquilo C3-6; o R1,1,3 y R1,1,4 junto con el átomo de N, al que están unidos, forman un anillo heterocíclico de 4, 5 o 6 miembros que puede contener adicionalmente otro heteroátomo seleccionado de N, O y S, o R1,1,3 y R1,1,4 junto con el átomo de N, al que están unidos, forman una imida cíclica; R1,1,4,1 de modo independiente entre sí, halogeno, -NH2, -NH(alquilo C1-4), -N(alquilo C1-4)2 o -SO2-R1,1,2; R1,2 es halogeno, -NO2, -CN o fenilo; R1,3 es (a) halogeno, -NO2, -CN, -OR1,1,1, -SR1,1,1, -CO2R1,1,1, alquilo C1-6 o (b) alquilo C1-3, en el que cada grupo metileno está sustituido con hasta dos átomos de fluor y cada grupo metilo está sustituido con hasta tres átomos de fluor; R1,4 es, de modo independiente entre sí, (a) halogeno, -NO2, -CN, -OR1,1,1, -SR1,1,1, -S(O)-R1,1,2, -S(O)2-R1,1,2, -NR1,1,3R1,1,4, alquilo C1-6, (b) alquilo C1-3, en el que cada grupo metileno está sustituido con hasta dos átomos de fluor y cada grupo metilo está sustituido con hasta tres átomos de fluor, o (c) un grupo oxo; R2 es (a) H, alquilo C1-4 o (b) alquilo C1-3, en el que cada grupo metileno está sustituido con hasta dos átomos de fluor y cada grupo metilo está sustituido con hasta tres átomos de fluor; R3 es, de modo independiente entre sí, (a) H, halogeno, -CN, -OH, alquilo C1-6, cicloalquilo C3-7, -O-alquilo C1-4, -O-CF3, -O-cicloalquilo C3-6, -N(alquilo C1-3)2, -C(O)-NH2, -(SO2)NH2, -SO2-alquilo C1-3, o (b) alquilo C1-3, en el que cada grupo metileno está sustituido con hasta dos átomos de fluor y cada grupo metilo está sustituido con hasta tres átomos de fluor; R4, R5, R6, R7, R8 son, de modo independiente entre sí, (a) H, halogeno, -CN, -OH, (b) alquilo C1-6, en donde dos sustituyentes adyacentes pueden representar juntos un grupo trimetileno o tetrametileno, (c) alquilo C1-3 en el que cada grupo metileno está sustituido con hasta dos átomos de fluor y cada grupo metilo está sustituido con hasta tres átomos de fluor, (d) cicloalquilo C3-7, (e) -O-alquilo C1-6, en donde dos sustituyentes adyacentes pueden representar un grupo metilendioxi o etilendioxi, (f) -O-CF3, -O-cicloalquilo C3-7, (g) -NH2, -NH(alquilo C1-3), -N(alquilo C1-3)2, (h) -C(O)-R8,1, (i) -SO2R8,2, (j) un grupo heteroarilo de cinco miembros eventualmente sustituido con uno o dos grupos alquilo C1-3, que está seleccionado del grupo compuesto por pirrolilo, oxazolilo, isoxazolilo, oxadiazolilo, tiazolilo, isotiazolilo, tiadiazolilo, imidazolilo, pirazolilo, triazolilo y tetrazolilo o (k) un grupo heteroarilo de seis miembros eventualmente sustituido con uno o dos grupos alquilo C1-3, que está seleccionado del grupo compuesto por piridilo, pirimidinilo, pirazinilo, piridazinilo y triazinilo; R8,1 es -NH2, -NH(alquilo C1-6), -N(alquilo C1-6)2, N-acetidinilo, N-pirrolidinilo, N-piperidinilo, N-morfolinilo, -OH, -O-alquilo C1-8 u -O-cicloalquilo C3-7; R8,2 es -NH2, -NH(alquilo C1-6), -N(alquilo C1-6)2, N-acetidinilo, N-pirrolidinilo, N-piperidinilo o N-morfolinilo; y n es una de las cifras 0, 1, 2, 3 o 4; sus enantiomeros, sus diastereoisomeros, sus mezclas y sus sales, en particular sus sales fisiologicamente compatibles con ácidos o bases orgánicos o inorgánicos. Reivindicacion 16: Sales fisiologicamente compatibles de los compuestos segun una de las reivindicaciones 1 a 15 caracterizadas porque son sales con ácidos o bases inorgánicos u orgánicos. Reivindicacion 17: Medicamento, caracterizado porque contiene un compuesto segun al menos una de las reivindicaciones 1 a 15 o una sal fisiologicamente compatible segun la reivindicacion 16, eventualmente junto a una o varias sustancias de soporte y/o agentes diluyentes inertes. Reivindicacion 18: Uso de un compuesto de acuerdo con al menos una de las reivindicaciones 1 a 16 caracterizado porque es para preparar un medicamento para el tratamiento agudo y preventivo de dolores agudos, dolores viscerales, dolores neuropáticos, dolores inflamatorios / mediados por el receptor del dolor, dolores tumorales y afecciones de cefaleas. Reivindicacion 19: Procedimiento para la preparacion de un medicamento segun la reivindicacion 17, caracterizado porque, por vía no química, un compuesto segun al menos una de las reivindicaciones 1 a 16 se incorpora en una o varias sustancias de soporte y/o agentes diluyentes inertes.
ARP080103747A 2007-08-29 2008-08-28 Compuestos b1-antagonistas, sus sales farmaceuticamente compatibles, medicamentos que contienen dichos compuestos, uso de los mismos para preparar medicamentos y procedimientoo de preparacion de un medicamento AR070750A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE102007041042 2007-08-29

Publications (1)

Publication Number Publication Date
AR070750A1 true AR070750A1 (es) 2010-05-05

Family

ID=40058897

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP080103747A AR070750A1 (es) 2007-08-29 2008-08-28 Compuestos b1-antagonistas, sus sales farmaceuticamente compatibles, medicamentos que contienen dichos compuestos, uso de los mismos para preparar medicamentos y procedimientoo de preparacion de un medicamento

Country Status (9)

Country Link
US (1) US8916589B2 (es)
EP (1) EP2188254B1 (es)
JP (1) JP5238812B2 (es)
AR (1) AR070750A1 (es)
AT (1) ATE550321T1 (es)
CA (1) CA2697946C (es)
CL (1) CL2008002545A1 (es)
TW (1) TW200911761A (es)
WO (1) WO2009027450A1 (es)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE102007034620A1 (de) * 2007-07-25 2009-01-29 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue B1-Antagonisten
ME01526B (me) * 2009-02-26 2014-04-20 Boehringer Ingelheim Int Jedinjenja kao b1 antagonisti bradikinina
WO2010097373A1 (de) * 2009-02-26 2010-09-02 Boehringer Ingelheim International Gmbh Verbindungen als bradykinin b1 antagonisten
WO2010097374A1 (de) * 2009-02-26 2010-09-02 Boehringer Ingelheim International Gmbh Verbindungen als bradykinin-b1-antagonisten
SG175711A1 (en) * 2009-05-18 2011-12-29 Orion Corp Protease inhibitors
US8937073B2 (en) 2010-08-20 2015-01-20 Boehringer Ingelheim International Gmbh Disubstituted tetrahydrofuranyl compounds and their use as B1-receptor antagonists
WO2012022794A1 (de) 2010-08-20 2012-02-23 Boehringer Ingelheim International Gmbh Pyridazinderivative als bradykinin b1 rezeptor antagonsiten
US20220235013A1 (en) 2017-03-21 2022-07-28 Bayer Pharma Aktiengesellschaft 2-methyl-quinazolines
CA3097231A1 (en) 2018-04-18 2019-10-24 Bayer Pharma Aktiengesellschaft 2-methyl-aza-quinazolines
EP3696159A1 (en) * 2019-02-14 2020-08-19 BASF Agro B.V. Process for the preparation of substituted phenoxyphenyl ketones

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP4342937B2 (ja) 2001-07-03 2009-10-14 バーテックス ファーマシューティカルズ インコーポレイテッド ＳｒｃおよびＬｃｋタンパク質キナーゼの阻害剤としてのイソキサゾールピリミジン
ES2256727T3 (es) 2002-02-08 2006-07-16 MERCK & CO., INC. Derivados de n-bifenilmetil aminocicloalcanocarboxamida.
US6919343B2 (en) * 2002-02-08 2005-07-19 Merck & Co., Inc. N-biphenyl(substituted methyl) aminocycloalkane-carboxamide derivatives
BR0313239A (pt) 2002-08-29 2005-06-14 Merck & Co Inc Composto, composição farmacêutica, e, métodos de tratamento ou prevenção de dor e inflamação e de doenças
US7332499B2 (en) 2003-08-07 2008-02-19 Merck & Co., Inc. Sulfonyl substituted n-(biarylmethyl) aminocyclopropanecarboxamides
EP1723143B1 (en) 2004-03-02 2009-02-18 Merck & Co., Inc. Amino cyclopropane carboxamide derivatives as bradykinin antagonists
HUP0600809A3 (en) 2006-10-27 2008-09-29 Richter Gedeon Nyrt New phenylsulfamoyl-benzamide derivatives as bradykinin antagonists, process and intermediates for their preparation and pharmaceutical compositions containing them
US20080227823A1 (en) * 2007-03-12 2008-09-18 Hassan Pajouhesh Amide derivatives as calcium channel blockers
DE102007034620A1 (de) 2007-07-25 2009-01-29 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue B1-Antagonisten
EP2025675A1 (de) 2007-08-14 2009-02-18 Boehringer Ingelheim International GmbH Arylsulfonamide mit analgetischer Wirkung
ME01526B (me) 2009-02-26 2014-04-20 Boehringer Ingelheim Int Jedinjenja kao b1 antagonisti bradikinina
SG183336A1 (en) 2010-02-23 2012-09-27 Boehringer Ingelheim Int Compounds as bradykinin b1 antagonists
US8937073B2 (en) 2010-08-20 2015-01-20 Boehringer Ingelheim International Gmbh Disubstituted tetrahydrofuranyl compounds and their use as B1-receptor antagonists
WO2012022794A1 (de) 2010-08-20 2012-02-23 Boehringer Ingelheim International Gmbh Pyridazinderivative als bradykinin b1 rezeptor antagonsiten

Also Published As

Publication number Publication date
EP2188254B1 (de) 2012-03-21
CL2008002545A1 (es) 2009-10-23
CA2697946A1 (en) 2009-03-05
ATE550321T1 (de) 2012-04-15
CA2697946C (en) 2016-06-28
JP2010536930A (ja) 2010-12-02
US20110263626A1 (en) 2011-10-27
JP5238812B2 (ja) 2013-07-17
WO2009027450A1 (de) 2009-03-05
TW200911761A (en) 2009-03-16
US8916589B2 (en) 2014-12-23
EP2188254A1 (de) 2010-05-26

Similar Documents

Publication Publication Date Title
AR070750A1 (es) Compuestos b1-antagonistas, sus sales farmaceuticamente compatibles, medicamentos que contienen dichos compuestos, uso de los mismos para preparar medicamentos y procedimientoo de preparacion de un medicamento
AR127309A2 (es) Derivados de piridazinona
AR075599A1 (es) Amidas derivadas de acidos heterociclicos, medicamentos que las contienen y uso de las mismas para el tratamiento agudo y preventivo de distintos tipos de dolores.
AR088029A1 (es) Compuestos de pirimidina sustituidos, composiciones farmaceuticas que los contienen y uso de los mismos para el tratamiento del dolor, accidentes cerebrovasculares, epilepsia y otras enfermedades del sistema nervioso central
AR100691A1 (es) Esteroides neuroactivos, composiciones, y usos de los mismos
AR069412A1 (es) Derivados de pirimidina, proceso para prepararlos, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de enfermedades virales, bacterianas y alergicas, entre otras.
AR069174A1 (es) Derivados de pirazolo[3,4-b]-piridina inhibidores de proteinquinasas, procesos de preparacion, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de enfermedades autoinmunes, inflamatorias o proliferativas.
AR087196A1 (es) Metodos plaguicidas que utilizan compuestos de 3-piridil tiazol sustituido y derivados para combatir las plagas de animales ii
AR112216A1 (es) Derivados de azaquinolina
AR064454A1 (es) Derivados de pirazol con efecto inhibitorio de fgfr, metodos para su sintesis, composicion farmaceutica que los comprende, un proceso para la preparacion de la misma y su uso en la fabricacion de un medicamento para el tratamiento del cancer.
AR063602A1 (es) Derivados de espiroindolinona, formulaciones farmaceuticas que los contienen y su uso en la obtencion de un medicamento para el tratamiento de trastornos oncologicos.
AR100806A1 (es) Inhibidores de fosfatidilinositol 3-quinasa
AR100810A1 (es) Inhibidores de fosfatidilinositol 3-quinasa
AR078535A1 (es) Derivados de pirrolo[2,3-b]piridina ligandos de receptores estrogenicos, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de la osteoporosis y enfermedades del sistema nervioso central, entre otras
AR067093A1 (es) N-(2-(hetaril) arilsulfonamidas y n-(2-( heteraril) hetaril) arilsulfonamidas
EA201791254A1 (ru) Кристаллические сольваты и комплексы производных (1s)-1,5-ангидро-1-c-(3-((фенил)метил)фенил)-d-глюцитола с аминокислотами в качестве ингибиторов sglt2 для лечения диабета
AR061815A1 (es) Compuesto de oxo-prolinamida composicion farmaceutica que lo comprende y su uso para la elaboracion de un medicamento
AR052943A1 (es) Derivados de 2-(4-oxo-4h-quinazolin-3-il)acetamida
AR082763A1 (es) Derivados de piperidinona como inhibidores mdm2 para el tratamiento de cancer
PE20161035A1 (es) Compuestos y usos de estos para la modulacion de la hemoglobina
AR045040A1 (es) Derivados de compuestos espiroazabiciclicos, composiciones farmaceuticas que los contienen y su uso en la preparacion de medicamentos
AR062737A1 (es) Composicion farmaceutica que comprende un compuesto derivado de aril-azabiciclo, compuesto correspondiente y su uso para la preparacion de un medicamento
PE20220386A1 (es) Amidas de pirazolo-piridina sustituidas y su uso como moduladores del receptor glun2b
AR087211A1 (es) ANTAGONISTAS DE CRTh2
AR069813A1 (es) Derivados de 2- amino-pirimidina, una composicion farmaceutica, un metodo de preparacion del compuesto y uso del mismo para preparar un medicamento

Legal Events

Date Code Title Description
FB Suspension of granting procedure