[go: up one dir, main page]

AR056544A1 - Derivados fenilaminopropanol y metodos de uso de los mismos - Google Patents

Derivados fenilaminopropanol y metodos de uso de los mismos

Info

Publication number
AR056544A1
AR056544A1 ARP060104236A ARP060104236A AR056544A1 AR 056544 A1 AR056544 A1 AR 056544A1 AR P060104236 A ARP060104236 A AR P060104236A AR P060104236 A ARP060104236 A AR P060104236A AR 056544 A1 AR056544 A1 AR 056544A1
Authority
AR
Argentina
Prior art keywords
substituted
alkyl
ring
exists
atoms
Prior art date
Application number
ARP060104236A
Other languages
English (en)
Original Assignee
Wyeth Corp
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=37697905&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR056544(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Wyeth Corp filed Critical Wyeth Corp
Publication of AR056544A1 publication Critical patent/AR056544A1/es

Links

Classifications

    • 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
    • C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • 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
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • 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
    • A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • A61P25/24—Antidepressants
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/12—Antidiuretics, e.g. drugs for diabetes insipidus
    • 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
    • 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
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • 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
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/12—Radicals substituted by oxygen atoms
    • 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
    • C07D209/32—Oxygen atoms
    • C07D209/34—Oxygen atoms in position 2
    • 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
    • C07D209/56—Ring systems containing three or more rings
    • C07D209/96—Spiro-condensed ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles 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 in position 2
    • C07D235/26—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/36—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems
    • C07D241/38—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems with only hydrogen or carbon atoms directly attached to the ring nitrogen atoms
    • C07D241/40—Benzopyrazines
    • C07D241/42—Benzopyrazines with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
    • 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
    • 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)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Endocrinology (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Reproductive Health (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Gynecology & Obstetrics (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Psychiatry (AREA)
  • Anesthesiology (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Obesity (AREA)
  • Emergency Medicine (AREA)
  • Pregnancy & Childbirth (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Las composiciones que contienen estos derivados y los métodos de uso, para la prevencion y tratamiento de las condiciones que se mejoran a través de la recaptacion de monoamina inter alia incluyendo entre otras, a los síntomas vasomotores (VMS), disfuncion sexual, desordenes gastrointestinales y genitourinarios, síndrome de fatiga cronica, síndrome de fibromialgia, desordenes del sistema nervioso, y combinaciones de lo mismo, particularmente aquellas condiciones seleccionadas del grupo que consiste de desorden depresivo mayor, síntomas vasomotores, incontinencia urinaria por estrés e incontinencia urinaria por urgencia, fibromialgia, dolor, neuropatía diabética, esquizofrenia, y combinaciones de lo mismo. Reivindicacion 1: Un compuesto de formula (1) o una sal farmacéuticamente aceptable de lo mismo; caracterizado porque la línea punteada entre Y y Z representa un segundo enlace opcional; la línea punteada entre los dos grupos R4 representa un anillo heterociclo opcional de 4 a 6 átomos en el anillo que se puede formar entre los dos grupos R4 grupos, junto con el N a través del cual están unidos; X es -(C(R12)2)o-, -O(C(R12)2)o-, -(C(R12)2)oO-, -S(O)p(C(R12)2)o-, -(C(R12)2)oS(O)p-, -N(R13)C(O)(C(R12)2)o-, - (C(R12)2)oC(O)N(R13)-, -C(O)N(R13)(C(R12)2)o-, -(C(R12)2)oN(R13)C(O)-, -(C(R12)2)oN(R13)S(O)2-, -S(O)2N(R13)(C(R12)2)o-, -N(R13)S(O)2(C(R12)2)o-, -(C(R12)2)oS(O)2N(R13)-, -NR7(C(R12)2)o-, -(C(R12)2)oNR7-, o -C:::C-; Y es N, C(R6)2, CR6, o C=O; Z es O, S(O)p, N, NR7, CR5, o C(R5)2; R1 es, independientemente cada vez que existe, alquilo, alcoxi halogeno, CF3, OCF3, hidroxi, alcanoiloxi, nitro, ciano, alquenilo, alquinilo, alquilsulfoxido, alquilsulfona, alquilsulfonamida, o alquilamido, o dos R1 adyacentes también representan metilendioxi; R2 es arilo sustituido con 0-3 R14 o heteroarilo sustituido con 0-3 R14; R3 es H o C1-4 alquilo; R4 es, independientemente cada vez que existe, H, C1-4 alquilo, C3-6 cicloalquilo, arilalquilo, hetero- arilmetilo, cicloheptilmetilo, ciclohexilmetilo, ciclopentilmetilo, o ciclobutilmetilo, o ambos grupos R4, junto con el N a través del cual están unidos, forman un anillo heterocíclico de 4 a 6 átomos en el anillo, donde un C puede estar opcionalmente reemplazado con N, O, S, o SO2, y donde cualquier átomo de C del anillo o átomo de N adicional puede estar opcionalmente sustituido con C1-4 alquilo, F, o CF3; R5 es, independientemente cada vez que existe, H, C1-4 alquilo, arilo sustituido con 0-3 R14, heteroarilo sustituido con 0-3 R14, ciano; o cuando dos R5 están presentes, estos pueden formar un anillo carbocíclico de 3-5 C; R6 es, independientemente cada vez que existe, H, C1-4 alquilo, o ciano; R7 es H, C1-6 alquilo, C3-6 cicloalquilo, arilo sustituido con 0-3 R14; o heteroarilo sustituido con 0-3 R14; R8 es H, o C1-4 alquilo; R9 es H, o C1-4 alquilo; R10 es, independientemente cada vez que existe, H, o C1-4 alquilo; o R10 y R4 junto con el N al cual R4 está unido forma un anillo que contiene N que a la vez contiene 3-6 átomos de C; R11 es arilo sustituido con 0-3 R1 o heteroarilo sustituido con 0-3 R1; R12 es, independientemente cada vez que existe, H, C1-4 alquilo; R13 es H o C1-4 alquilo; R14 es, independientemente cada vez que existe, alquilo, alcoxi, halogeno, CF3, OCF3, arilalquiloxi sustituido con 0-3 R1, ariloxi sustituido con 0-3 R1, arilo sustituido con 0-3 R1, heteroarilo sustituido con 0-3 R1, hidroxi, alcanoiloxi, nitro, ciano, alquenilo, alquinilo, alquilsulfoxido, fenilsulfoxido sustituido con 0-3 R1, alquilsulfona, fenilsulfona sustituida con 0-3 R1, alquilsulfonamida, fenilsulfonamida sustituida con 0-3 R1, heteroariloxi sustituido con 0-3 R1, heteroarilmetiloxi sustituido con 0-3 R1, alquilamido, o arilamido sustituido con 0-3 R1, o dos R1 adyacentes también representan metilendioxi; m es un numero entero desde 0 a 3; n es un numero entero desde 1 a 2; o es un numero entero desde 0 a 3; y p es un numero entero desde 0 a 2; donde 1-3 átomos de C en el anillo A pueden opcionalmente estar reemplazados con N. Reivindicacion 22: Un compuesto de formula (2) o una sal farmacéuticamente aceptable de los mismo; caracterizado porque D y E, junto con el átomo de C a través del cual están unidos, forman un anillo carbocíclico de 6 a 8 átomos o un anillo heterocíclico de 5 a 8 átomos que contiene 1 a 2 heteroátomos seleccionados de O, S(O)p, y NR7, donde cualquier átomo de C en el anillo puede estar opcionalmente sustituido con C1-4 alquilo, F, o CF3; la línea punteada entre los dos grupos R4 representan un anillo heterociclo opcional de 4 a 6 átomos en el anillo que se puede formar entre los dos grupos R4, junto con el N a través del cual están unidos; G es NR7, C(R6)2, o C=O; R1 es, independientemente cada vez que existe, alquilo, alcoxi, halogeno, CF3, OCF3, hidroxi, alcanoiloxi, nitro, ciano, alquenilo, alquinilo, alquilsulfoxido, alquilsulfona, alquilsulfonamida, o alquilamido; o dos R1 adyacentes también representan metilendioxi; R2 es arilo sustituido con 0-3 R14 o heteroarilo sustituido con 0-3 R14; R3 es H o C1-4 alquilo; R4 es, independientemente cada vez que existe, H, C1-4 alquilo, C3-6 cicloalquilo, arilalquilo, heteroaril-metilo, cicloheptilmetilo, ciclohexilmetilo, ciclopentilmetilo, o ciclobutilmetilo, o ambos grupos R4, junto con el N a través del cual están unidos, forman un anillo heterocíclico de 4 a 6 átomos en el anillo, donde un C puede estar opcionalmente reemplazado con N, O, S, o SO2, y donde cualquier átomo deC del anillo o átomo de N adicional puede estar opcionalmente sustituido con C1-4 alquilo, F, o CF3; R6 es, independientemente cada vez que existe, H, C1-4 alquilo, o ciano; R7 es H, C1-6 alquilo, C3-6 cicloalquilo, arilo sustituido con 0-3 R14; o heteroarilo sustituido con 0-3 R14; R8 es H, o C1-4 alquilo; R9 es H, o C1-4 alquilo; R10 es, independientemente cada vez que existe, H, o C1-4 alquilo; o R10 y R4 junto con el N al cual R4 está unido forma un anillo que contiene N que a la vez contiene 3-6 átomos de C; R14 es, independientemente cada vez que existe, alquilo, alcoxi, halogeno, CF3, OCF3, arilalquiloxi sustituido con 0-3 R1, ariloxi sustituido con 0-3 R1, arilo sustituido con 0-3 R1, heteroarilo sustituido con 0-3 R1, hidroxi, alcanoiloxi, nitro, ciano, alquenilo, alquinilo, alquilsulfoxido, fenilsulfoxido sustituido con 0-3 R1, alquilsulfona, fenilsulfona sustituida con 0-3 R1, alquilsulfonamida, fenilsulfonamida sustituida con 0-3 R1, heteroariloxi sustituido con 0-3 R1, heteroarilmetiloxi sustituido con 0-3 R1, alquilamido, o arilamido sustituido con 0-3 R1, o dos R1 adyacentes también representan metilendioxi; n es un numero entero desde 1 a 2; p es un numero entero desde 0 a 2; y q es un numero entero desde 0 a 4; donde 1-3 átomos de C en el anillo A pueden opcionalmente estar reemplazados con N. Reivindicacion 36: Un compuesto de formula (3), o una sal farmacéuticamente aceptable de lo mismo; caracterizado porque la línea punteada entre Y y Z representa un segundo enlace opcional; la línea punteada entre los dos grupos R4 representa un anillo heterociclo opcional de 4 a 6 átomos en el anillo que se puede formar entre los dos grupos R4, junto con el N a través del cual están unidos; Y es N, C(R6)2, CR6, o C=O; Z es O, S(O)p, N, NR7, CR5, o C(R5)2; R1 es, independientemente cada vez que existe, alquilo, alcoxi, halogeno, CF3, OCF3, hidroxi, alcanoiloxi, nitro, ciano, alquenilo, alquinilo, alquilsulfoxido, alquilsulfona, alquilsulfonamida, o alquilamido; o dos R1 adyacentes también representan metilendioxi; R2 es arilo sustituido con 0-3 R14 o heteroarilo sustituido con 0-3 R14; R3 es H o C1-4 alquilo; R4 es, independientemente cada vez que existe, H, C1-4 alquilo, C3-6 cicloalquilo, arilalquilo, heteroaril-metilo, cicloheptilmetilo, ciclohexilmetilo, ciclopentilmetilo, o ciclobutilmetilo, o ambos grupos R4, junto con el N a través del cual están unidos, forman un anillo heterocíclico de 4 a 6 átomos en el anillo, donde un C puede estar opcionalmente reemplazado con N, O, S, o SO2, y donde cualquier átomo deC del anillo o átomo de N adicional puede estar opcionalmente sustituido con C1-4 alquilo, F, o CF3; R5 es, independientemente cada vez que existe, H, C1-4 alquilo, arilo sustituido con 0-3 R14, heteroarilo sustituido con 0-3 R14, ciano; o cuando dos R5 están presentes, estos pueden formar un anillo carbocíclico de 3-5 C; R6 es, independientemente cada vez que existe, H, C1-4 alquilo, o ciano; R7 es H, C1-6 alquilo, C3-6 cicloalquilo, arilo sustituido con 0-3 R14; o heteroarilo sustituido con 0-3 R14; R8 es H, o C1-4 alquilo; R9 es H, o C1-4 alquilo; R10 es, independientemente cada vez que existe, H, o C1-4 alquilo; o R10 y R4 junto con el N al cual R4 está unido forma un anillo que contiene N que a la vez contiene 3-6 átomos de C; R14 es, independientemente cada vez que existe, alquilo, alcoxi, halogeno, CF3, OCF3, arilalquiloxi sustituido con 0-3 R1, ariloxi sustituido con 0-3 R1, arilo sustituido con 0-3 R1, heteroarilo sustituido con 0-3 R1, hidroxi, alcanoiloxi, nitro, ciano, alquenilo, alquinilo, alquilsulfoxido, fenilsulfoxido sustituido con 0-3 R1, alquilsulfona, fenilsulfona sustituida con 0-3 R1, alquilsulfonamida, fenilsulfonamida sustituida con 0-3 R1, heteroariloxi sustituido con 0-3 R1, heteroarilmetiloxi sustituido con 0-3 R1, alquilamido, o arilamido sustituido con 0-3 R1, o dos R1 adyacentes también representan metilendioxi; n es un numero entero desde 1 a 2; y q es un numero entero desde 0 a 4; donde 1-3 átomos de C en el anillo A pueden opcionalmente estar reemplazados con N.
ARP060104236A 2005-09-29 2006-09-27 Derivados fenilaminopropanol y metodos de uso de los mismos AR056544A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US72167605P 2005-09-29 2005-09-29

Publications (1)

Publication Number Publication Date
AR056544A1 true AR056544A1 (es) 2007-10-10

Family

ID=37697905

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP060104236A AR056544A1 (es) 2005-09-29 2006-09-27 Derivados fenilaminopropanol y metodos de uso de los mismos

Country Status (11)

Country Link
US (1) US20070072897A1 (es)
EP (1) EP1931631A1 (es)
JP (1) JP2009510066A (es)
CN (1) CN101309904A (es)
AR (1) AR056544A1 (es)
AU (1) AU2006297414A1 (es)
BR (1) BRPI0616459A2 (es)
CA (1) CA2624220A1 (es)
PE (1) PE20070462A1 (es)
TW (1) TW200800887A (es)
WO (1) WO2007041023A1 (es)

Families Citing this family (54)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8595055B2 (en) 2001-03-27 2013-11-26 Points.Com Apparatus and method of facilitating the exchange of points between selected entities
EP1831225A2 (en) * 2004-11-19 2007-09-12 The Regents of the University of California Anti-inflammatory pyrazolopyrimidines
WO2007062998A1 (en) * 2005-11-30 2007-06-07 F. Hoffmann-La Roche Ag 3-amino-2-arylpropyl azaindoles and uses thereof
KR20130087054A (ko) 2006-04-04 2013-08-05 더 리젠트스 오브 더 유니이버시티 오브 캘리포니아 키나제 길항물질
EP2865381A1 (en) * 2006-05-18 2015-04-29 Pharmacyclics, Inc. ITK inhibitors for treating blood cell malignancies
TW200817382A (en) * 2006-08-24 2008-04-16 Wyeth Corp Process for preparing indolinone phenylaminopropanol derivatives
WO2009046448A1 (en) 2007-10-04 2009-04-09 Intellikine, Inc. Chemical entities and therapeutic uses thereof
US8193182B2 (en) 2008-01-04 2012-06-05 Intellikine, Inc. Substituted isoquinolin-1(2H)-ones, and methods of use thereof
JP5869222B2 (ja) 2008-01-04 2016-02-24 インテリカイン， エルエルシー 特定の化学的実体、組成物および方法
US8993580B2 (en) 2008-03-14 2015-03-31 Intellikine Llc Benzothiazole kinase inhibitors and methods of use
WO2009114870A2 (en) * 2008-03-14 2009-09-17 Intellikine, Inc. Kinase inhibitors and methods of use
DE102008022221A1 (de) 2008-05-06 2009-11-12 Universität des Saarlandes Inhibitoren der humanen Aldosteronsynthase CYP11B2
JP5527668B2 (ja) * 2008-06-05 2014-06-18 エスケー バイオファーマスティカルズ カンパニー リミテッド ３−置換プロパンアミン化合物
WO2010006072A2 (en) 2008-07-08 2010-01-14 The Regents Of The University Of California Mtor modulators and uses thereof
BRPI0915231A2 (pt) * 2008-07-08 2018-06-12 Intellikine Inc compostos inibidores de quinase e métodos de uso
CA2738429C (en) 2008-09-26 2016-10-25 Intellikine, Inc. Heterocyclic kinase inhibitors
JP5819195B2 (ja) 2008-10-16 2015-11-18 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア 融合環ヘテロアリールキナーゼ阻害剤
US8476431B2 (en) 2008-11-03 2013-07-02 Itellikine LLC Benzoxazole kinase inhibitors and methods of use
CA2760791C (en) 2009-05-07 2017-06-20 Intellikine, Inc. Heterocyclic compounds and uses thereof
CN102573836A (zh) * 2009-06-10 2012-07-11 雅培股份有限两合公司 取代的羟吲哚衍生物治疗和预防疼痛的应用
PE20170003A1 (es) 2009-08-17 2017-03-15 Intellikine Llc Compuestos heterociclicos y usos de los mismos
US8980899B2 (en) 2009-10-16 2015-03-17 The Regents Of The University Of California Methods of inhibiting Ire1
US8541404B2 (en) * 2009-11-09 2013-09-24 Elexopharm Gmbh Inhibitors of the human aldosterone synthase CYP11B2
EP3381899B1 (en) * 2010-04-22 2021-01-06 Vertex Pharmaceuticals Incorporated Intermediate compound for process of producing cycloalkylcarboxamido-indole compounds
EP2571357B1 (en) 2010-05-21 2016-07-06 Infinity Pharmaceuticals, Inc. Chemical compounds, compositions and methods for kinase modulation
CN103298474B (zh) 2010-11-10 2016-06-29 无限药品股份有限公司 杂环化合物及其用途
HUE030393T2 (en) 2010-12-28 2017-05-29 Sanofi Sa New pyrimidine derivatives, a process for their preparation, and their pharmaceutical use as inhibitors of AKT (PKB) phosphorylation
MX347708B (es) 2011-01-10 2017-05-09 Infinity Pharmaceuticals Inc Proceso para preparar isoquinolinonas y formas solidas de isoquinolinonas.
EP2665707B1 (en) * 2011-01-20 2017-01-18 Merck Sharp & Dohme Corp. Mineralocorticoid receptor antagonists
EP2678018A4 (en) 2011-02-23 2015-09-30 Intellikine Llc COMBINATION OF CHINESE HEMMER AND USES THEREOF
AU2012284088B2 (en) 2011-07-19 2015-10-08 Infinity Pharmaceuticals Inc. Heterocyclic compounds and uses thereof
CN103946226A (zh) 2011-07-19 2014-07-23 无限药品股份有限公司 杂环化合物及其应用
HK1199725A1 (en) 2011-08-29 2015-07-17 无限药品股份有限公司 Heterocyclic compounds and uses thereof
WO2013077921A2 (en) 2011-09-02 2013-05-30 The Regents Of The University Of California Substituted pyrazolo[3,4-d]pyrimidines and uses thereof
US8940742B2 (en) 2012-04-10 2015-01-27 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
US8828998B2 (en) 2012-06-25 2014-09-09 Infinity Pharmaceuticals, Inc. Treatment of lupus, fibrotic conditions, and inflammatory myopathies and other disorders using PI3 kinase inhibitors
WO2014052669A1 (en) 2012-09-26 2014-04-03 The Regents Of The University Of California Modulation of ire1
RU2702908C2 (ru) 2012-11-01 2019-10-14 Инфинити Фармасьютикалз, Инк. Лечение злокачественных опухолей с использованием модуляторов изоформ pi3-киназы
US9481667B2 (en) 2013-03-15 2016-11-01 Infinity Pharmaceuticals, Inc. Salts and solid forms of isoquinolinones and composition comprising and methods of using the same
CA2907726A1 (en) 2013-03-22 2014-09-25 Millennium Pharmaceuticals, Inc. Combination of catalytic mtorc1/2 inhibitors and selective inhibitors of aurora a kinase
HUE057734T2 (hu) 2013-10-04 2022-06-28 Infinity Pharmaceuticals Inc Heterociklusos vegyületek és alkalmazásuk
WO2015051241A1 (en) 2013-10-04 2015-04-09 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
CN113616656B (zh) 2014-03-19 2023-02-17 无限药品股份有限公司 用于治疗PI3K-γ介导的障碍的杂环化合物
US20150320755A1 (en) 2014-04-16 2015-11-12 Infinity Pharmaceuticals, Inc. Combination therapies
WO2016054491A1 (en) 2014-10-03 2016-04-07 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
WO2016179157A1 (en) 2015-05-05 2016-11-10 Carafe Drug Innovation, Llc Substituted 5-hydroxyoxindoles and their use as analgesics and fever reducers
KR102704783B1 (ko) * 2015-05-18 2024-09-10 칸디 테라퓨틱스 리미티드 성-호르몬 의존성 질환의 치료를 위한 이중 nk-1/nk-3 수용체 길항제
EP3350183B1 (en) 2015-09-14 2025-04-02 Twelve Therapeutics, Inc. Solid forms of isoquinolinone derivatives, process of making, compositions comprising, and methods of using the same
WO2017161116A1 (en) 2016-03-17 2017-09-21 Infinity Pharmaceuticals, Inc. Isotopologues of isoquinolinone and quinazolinone compounds and uses thereof as pi3k kinase inhibitors
WO2017214269A1 (en) 2016-06-08 2017-12-14 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
MX391135B (es) 2016-06-24 2025-03-21 Infinity Pharmaceuticals Inc Terapias de combinacion.
CA3102279A1 (en) 2018-06-01 2019-12-05 Cornell University Combination therapy for pi3k-associated disease or disorder
JP2021529757A (ja) 2018-07-03 2021-11-04 ザ ボード オブ トラスティーズ オブ ザ ユニバーシティ オブ イリノイ 小胞体ストレス応答の活性剤
KR20240050788A (ko) 2022-10-12 2024-04-19 동국대학교 산학협력단 멜라토닌 유사체 및 이의 퇴행성 신경질환 예방 또는 치료 용도

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US529450A (en) * 1894-11-20 Josef kirchmann and kaspar schwinghammer
US528792A (en) * 1894-11-06 Cultivator-plow
US5948807A (en) * 1997-09-03 1999-09-07 Regents Of The University Of Minnesota Spiroindanamines and Spiroindanimides
TW528754B (en) * 1998-04-29 2003-04-21 Wyeth Corp Indolyl derivatibes as serotonergic agents
EP1660484B1 (en) * 2003-05-09 2008-08-27 F. Hoffmann-La Roche Ag Methyl indoles and methyl pyrrolopyridines as alpha-1 adrenergic agonists
US7517899B2 (en) * 2004-03-30 2009-04-14 Wyeth Phenylaminopropanol derivatives and methods of their use
US7414052B2 (en) * 2004-03-30 2008-08-19 Wyeth Phenylaminopropanol derivatives and methods of their use
ES2340180T3 (es) * 2004-06-01 2010-05-31 F.Hoffmann-La Roche Ag 3-amino-1-arilpropil-indoles como inhibidores de reabsorcion de monoaminas.

Also Published As

Publication number Publication date
WO2007041023A1 (en) 2007-04-12
BRPI0616459A2 (pt) 2011-06-21
EP1931631A1 (en) 2008-06-18
AU2006297414A1 (en) 2007-04-12
JP2009510066A (ja) 2009-03-12
PE20070462A1 (es) 2007-06-05
TW200800887A (en) 2008-01-01
CA2624220A1 (en) 2007-04-12
US20070072897A1 (en) 2007-03-29
CN101309904A (zh) 2008-11-19

Similar Documents

Publication Publication Date Title
AR056544A1 (es) Derivados fenilaminopropanol y metodos de uso de los mismos
AR110051A2 (es) Pirazolo[3,4-d]pirimidinas útiles para tratar trastornos respiratorios
AR022820A1 (es) Compuestos derivados de piridopiranoacepinas, en forma de isomeros geometricos u opticos puros o de mezcla de tales isomeros, procedimiento para su preparacion, medicamento y composicion farmaceutica.
AR049646A1 (es) Derivados de sulfamato y sulfamida utiles para el tratamiento de la epilepsia y trastornos relacionados
AR068511A1 (es) Tetrahidro[1,4'] bipiridinil-2'-onas sustituidas, composiciones farmaceuticas que las contienen y usos de las mismas para tratar o prevenir trastornos del sistema nervioso central
AR048675A1 (es) Derivados de 1-(1h-indol- 1-il)- 3- (4-metilpiperazin-1-il)-1- fenil propan 2 ol
AR063015A1 (es) Derivados de quinazolinona 5-sustituida y composiciones que los comprenden y metodos para utilizarlos en el tratamiento del cancer
AR082393A1 (es) Derivados de amina cis-tetrahidro-espiro(ciclohexan-1,1’-pirido[3,4-b]indol)-4
AR058287A1 (es) Derivados de isoquinolina y composicion farmaceutica
AR041260A1 (es) Piperazinas sustituidas por heterociclos para el tratamiento de la esquizofrenia
AR054799A1 (es) Derivados de oxindol
AR070925A1 (es) 4- hidroxipirimidina -5- carboxamida sustituidas, un procedimiento para el tratamiento preventivo de anemia, procedimiento para potenciar la produccion endogena de eritropoyetina, uso del compuesto en la fabricacion de un medicamento y composicion farmaceutica
AR048454A1 (es) Azaindoles utiles como inhibidores de las proteinas quinasas jak u otras proteinas quinasas
AR072962A1 (es) Derivados de pirimidin-4-ona sustituidos
AR041566A1 (es) Derivados de indol utiles para el tratamiento de enfermedades
PE20091100A1 (es) Nuevos compuestos 010
AR037489A1 (es) Quinolinas sustituidas y proceso para su preparacion
AR052902A1 (es) Derivados de piridazina, composicion farmaceutica que los contiene y su uso como agentes terapeuticos para enfermedades mediadas por la estearoil-coa desaturasa
PA8522001A1 (es) Pro - farmacos de derivados de 4- fenil - piridin.
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
AR036875A1 (es) Acidos hidroxamicos ciclicos como inhibidores de las metaloproteinasas de matriz y/o de la enzima de conversion del factor de necrosis de tumor alfa
AR038179A1 (es) Fenilsulfonamidas para uso terapeutico
AR069607A1 (es) Inhibidores de la estearoil-coa desaturasa
AR051467A1 (es) Derivados de aminopiridina con accion inhibitoria selectiva de la aurora quinasa a
ECSP13012416A (es) Derivados heterocíclicos fusionados como moduladores s1p

Legal Events

Date Code Title Description
FA Abandonment or withdrawal