[go: up one dir, main page]

AR069753A1 - Compuestos de 1,2,4-triazol y composiciones, utiles en la modulacion de los niveles de acido urico sanguineo - Google Patents

Compuestos de 1,2,4-triazol y composiciones, utiles en la modulacion de los niveles de acido urico sanguineo

Info

Publication number
AR069753A1
AR069753A1 ARP080105142A ARP080105142A AR069753A1 AR 069753 A1 AR069753 A1 AR 069753A1 AR P080105142 A ARP080105142 A AR P080105142A AR P080105142 A ARP080105142 A AR P080105142A AR 069753 A1 AR069753 A1 AR 069753A1
Authority
AR
Argentina
Prior art keywords
optionally substituted
alkyl
substituted
propyl
aryl
Prior art date
Application number
ARP080105142A
Other languages
English (en)
Original Assignee
Ardea Biosciences Inc
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=40679222&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR069753(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Ardea Biosciences Inc filed Critical Ardea Biosciences Inc
Publication of AR069753A1 publication Critical patent/AR069753A1/es

Links

Classifications

    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/7056—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • A61K31/7072—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7076—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P13/04—Drugs for disorders of the urinary system for urolithiasis
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • 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
    • A61P39/00—General protective or antinoxious agents
    • A61P39/02—Antidotes
    • 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
    • A61P5/18—Drugs for disorders of the endocrine system of the parathyroid hormones
    • A61P5/20—Drugs for disorders of the endocrine system of the parathyroid hormones for decreasing, blocking or antagonising the activity of PTH
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D235/28—Sulfur 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
    • C07D249/10—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles 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
    • C07D249/12—Oxygen or sulfur 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
    • C07D249/10—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles 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
    • C07D249/14—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/06—Pyrimidine radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/16—Purine radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H7/00—Compounds containing non-saccharide radicals linked to saccharide radicals by a carbon-to-carbon bond
    • C07H7/02—Acyclic radicals

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Molecular Biology (AREA)
  • Epidemiology (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Rheumatology (AREA)
  • Toxicology (AREA)
  • Emergency Medicine (AREA)
  • Immunology (AREA)
  • Dermatology (AREA)
  • Pain & Pain Management (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Vascular Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Un compuesto de la formula (3), o un metabolito, sal farmacéuticamente aceptable, solvato, éster, tautomero o profármaco de los mismos. Un compuesto de la formula (2), en donde el compuesto de la formula (2) es un 3-sustituido-5-bromo-4-(4-ciclopropilnaftalen-1-iI)-4H-1,2,4-triazol en donde el sustituyente en la posicion 3 es -RB, o una sal farmacéuticamente aceptable, solvato, o tautomero de los mismos. Una composicion farmacéutica que comprende: (i) un compuesto de la formula (1); o (ii) un compuesto de la formula (2); o (iii) un compuesto de la formula (3); o (iv) una combinacion de los mismos; en donde: X es CH o N; W es O, S, S(O), S(O)2, NH, N(alquilo opcionalmente sustituido), NC(O)(alquilo opcionalmente sustituido) o CH2; R1 es H, Cl, Br, I, NH2, metilo, etilo, n-propilo, i-propilo, metilo opcionalmente sustituido, etilo opcionalmente sustituido, n-propilo opcionalmente sustituido, i-propilo opcionalmente sustituido, CF3, CHF2 o CH2F; R3 y R3' se seleccionan independientemente de H y alquilo inferior, o R3 y R3' junto con el carbono al que se encuentran unidos forman un anillo de 4, 5, o 6 miembros, que contiene opcionalmente 1 o 2 heteroátomos seleccionados de N, S y O; R2 se selecciona del grupo de formulas (4); en donde la línea de puntos representa un enlace simple carbono-carbono o un enlace doble carbono-carbono; Q y Q' se seleccionan independientemente de N y CH; RP es metilo, etilo, propilo, i-propilo, ciclopropilo, ciclobutilo, ciclopentilo, ciclohexilo o ciclopropilmetilo; R8, R9 y R10 se seleccionan independientemente de H, F, Cl, Br, CH3, CF3, CFH2, CF2H, etilo, i-propilo, ciclopropilo, metoxi, OH, OCF3, NH2 y NHCH3; R11 es Cl, Br, I, CH3, CF3, metoxi, i-propilo, ciclopropilo, ter-butilo, ciclobutilo o metilo; y R12, R13, R14 y R15 son independientemente H o metilo; RB es -SCH2C(=O)R1a, -SCH2-tetrazolilo, -SCH2C(=O)NHOH, -SCH2C(=O)O-alquil-OC(=O)R3a, -SCH2C(=O)O-alquil-OC(=O)OR3a, -SCH2C(=O)O-alquil-OC(=O)NR4aR4b, o -SCH2C(O-alquilo)3; R1a es OR2a, SR3a, NR4aR4b, al menos un aminoácido, un péptido, un lípido, un fosfolípido, un glucosido, un nucleotido, un oligonucleotido, polietilenglicol, o una combinacion de los mismos, en donde R2a es alquilo C1-4 opcionalmente sustituido, alquilo C5-10 opcionalmente sustituido, heteroalquilo opcionalmente sustituido, cicloalquilo opcionalmente sustituido, heterocicloalquilo opcionalmente sustituido, arilo opcionalmente sustituido o heteroarilo opcionalmente sustituido; o R2a es un cation farmacéuticamente aceptable; o R2a es -[C(R5a)(R5b)]mR5c; R3a es hidrogeno, alquilo C1-10 opcionalmente sustituido, heteroalquilo opcionalmente sustituido, cicloalquilo opcionalmente sustituido, heterocicloalquilo opcionalmente sustituido, arilo opcionalmente sustituido, heteroarilo opcionalmente sustituido; o R3a es -[C(R5a)(R5b)]nR5c; R4a es hidrogeno, alquilo opcionalmente sustituido, heteroalquilo opcionalmente sustituido, cicloalquilo opcionalmente sustituido o heterocicloalquilo opcionalmente sustituido; y R4b es hidrogeno, alquilo opcionalmente sustituido, heteroalquilo opcionalmente sustituido, cicloalquilo opcionalmente sustituido o heterocicloalquilo opcionalmente sustituido; o R4b es -[C(R5a)(R5b)]nR5c, en donde cada R5a es independientemente hidrogeno, halogeno, ciano, nitro, al menos un aminoácido, un péptido, un lípido, un fosfolípido, un glicosido, un nucleosido, un nucleotido, oligonucleotido, polietilenglicol, -L-OH, -L-SH, -L-NH2, -L-alquilo C1-3 sustituido, -L-alquilo C4-9 opcionalmente sustituido, -L-alquenilo C2-5 opcionalmente sustituido, -L-alquinilo C2-5 opcionalmente sustituido, -L-heteroalquilo C2-5 opcionalmente sustituido, -L-cicloalquilo C3-7 opcionalmente sustituido, -L-cicloalquenilo C3-7 opcionalmente sustituido, -L-heterocicloalquilo C3-7 opcionalmente sustituido, -L-haloalquilo C1-4 opcionalmente sustituido, -L-alcoxi C1-4 opcionalmente sustituido, -L-alquilamina C1-4 opcionalmente sustituido, -L-di-alquilamina C1-4 opcionalmente sustituida, -L-arilo C5-7 opcionalmente sustituido, -L-heteroarilo C5-7 opcionalmente sustituido, o un resto del grupo de formulas (5); cada R5b es independientemente hidrogeno, halogeno, ciano, nitro, al menos un aminoácido, un péptido, un lípido, un fosfolípido, un glicosido, un nucleosido, un nucleotido, oligonucleotido, polietilenglicol, -L-OH, -L-SH, -L-NH2, -L-alquilo C1-3 sustituido, -L-alquilo C4-9 opcionalmente sustituido, -L-alquenilo C2-5 opcionalmente sustituido, -L-alquinilo C2-5 opcionalmente sustituido, -L-heteroalquilo C2-5 opcionalmente sustituido, -L-cicloalquilo C3-7 opcionalmente sustituido, -L-cicloalquenilo C3-7 opcionalmente sustituido, -L-heterocicloalquilo C3-7 opcionalmente sustituido, -L-haloalquilo C1-4 opcionalmente sustituido, -L-alcoxi C1-4 opcionalmente sustituido, -L-alquilamina C1-4 opcionalmente sustituido, -L-di-alquilamina C1-4 opcionalmente sustituida, -L-arilo C5-7 opcionalmente sustituido, -L-heteroarilo C5-7 opcionalmente sustituido, o un resto del grupo de formulas (5); cada R5c es independientemente hidrogeno, halogeno, ciano, nitro, al menos un aminoácido, un péptido, un lípido, un fosfolípido, un glicosido, un nucleosido, un nucleotido, oligonucleotido, polietilenglicol, -L-OH, -L-SH, -L-NH2, -L-alquilo C1-3 sustituido, -L-alquilo C4-9 opcionalmente sustituido, -L-alquenilo C2-5 opcionalmente sustituido, -L-alquinilo C2-5 opcionalmente sustituido, -L-heteroalquilo C2-5 opcionalmente sustituido, -L-cicloalquilo C3-7 opcionalmente sustituido, -L-cicloalquenilo C3-7 opcionalmente sustituido, -L-heterocicloalquilo C3-7 opcionalmente sustituido, -L-haloalquilo C1-4 opcionalmente sustituido, -L-alcoxi C1-4 opcionalmente sustituido, -L-alquilamina C1-4 opcionalmente sustituido, -L-di-alquilamina C1-4 opcionalmente sustituida, -L-arilo C5-7 opcionalmente sustituido, -L-heteroarilo C5-7 opcionalmente sustituido, o un resto del grupo de formulas (5); en donde L es un enlace, -C(O)-, -S(O) o -S(O)2; y1 es 0, 1, 2 o 3; Y es OH, OMe, COOH, SO3H, OSO3H, OS(O)2NH2, P(O)(OH)2, OP(O)(OH)2, OP(O)(OH)(O-alquilo C1-4) o NY2Y3Y4; en donde Y2 e Y3 son cada uno independientemente hidrogeno o metilo; o Y2 e Y3 se toman en conjunto con el nitrogeno al cual están unidas para formar un anillo de cinco o seis miembros que contiene opcionalmente un átomo de oxígeno o un segundo átomo de nitrogeno; e Y4 es un par de electrones o un átomo de oxígeno; m es 1, 2, 3 o 4; n es 0, 1, 2, 3, 4, 5, 6, 7, 8, 9 o 10; y en donde si R2a es -[C(R5a)(R5b)]mR5c entonces al menos uno de R5a, R5b y R5c no es hidrogeno; R4 es H, alquilo inferior, alquenilo inferior o alquinilo inferior; R5, R5', R6, R6' y R7 se seleccionan independientemente de H, F, Cl, Br, I, metilo, etilo, n-propilo, i-propilo, metilo sustituido, etilo sustituido, n-propilo sustituido, i-propilo sustituido, ciclopropilo, ciclobutilo, ciclopentilo, CF3, CHF2, CH2F, NH2, NHR', NR'R'', OR', SR', C(O)R', CO2H, una sal de CO2H, COOR', CONH2, CONHR', CONR'R'', SO3H, una sal de SO3H, S(O)2R', S(O)2NH2, S(O)2NHR', S(O)2NR'R'', arilo o un heterociclo, en donde R' es H, alquilo C1-3, alquilo C1-3 sustituido en donde dichos sustituyentes se seleccionan de CF3, OH, O-alquilo C1-3, CO-alquilo C1-3, COOH, COO-alquilo C1-3, NH2, NH-alquilo C1-3, N(alquilo C1-3)(alquilo C1-3), CONH-alquilo C1-3, arilo o un heterociclo; R'' es H, alquilo C1-3, alquilo C1-3 sustituido en donde dicho sustituyentes se seleccionan de CF3, OH, O-alquilo C1-3, CO-alquilo C1-3, COOH, COO-alquilo C1-3, NH2, NH-alquilo C1-3, N(alquilo C1-3)(alquilo C1-3), CONH-alquilo C1-3, arilo o un heterociclo; o R' y R'' conjuntamente con el átomo de nitrogeno al cual están unidos forman un anillo heterocíclico de 4, 5 o 6 miembros; o un metabolito, sal farmacéuticamente aceptable, solvato, éster, tautomero o profármaco del mismo; y (v) opcionalmente uno o más transportadores farmacéuticamente aceptables. También reivindica el método de uso.
ARP080105142A 2007-11-27 2008-11-26 Compuestos de 1,2,4-triazol y composiciones, utiles en la modulacion de los niveles de acido urico sanguineo AR069753A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US99057407P 2007-11-27 2007-11-27
US9438808P 2008-09-04 2008-09-04

Publications (1)

Publication Number Publication Date
AR069753A1 true AR069753A1 (es) 2010-02-17

Family

ID=40679222

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP080105142A AR069753A1 (es) 2007-11-27 2008-11-26 Compuestos de 1,2,4-triazol y composiciones, utiles en la modulacion de los niveles de acido urico sanguineo

Country Status (35)

Country Link
US (8) US8084483B2 (es)
EP (2) EP2842948A1 (es)
JP (3) JP5099794B2 (es)
KR (2) KR101291643B1 (es)
CN (3) CN103058944B (es)
AR (1) AR069753A1 (es)
AU (2) AU2008329673C1 (es)
BR (1) BRPI0819847B1 (es)
CA (1) CA2706858C (es)
CL (1) CL2008003529A1 (es)
CY (1) CY2019010I1 (es)
DK (1) DK2217577T3 (es)
EA (2) EA018193B3 (es)
EC (1) ECSP10010310A (es)
ES (1) ES2513390T3 (es)
HR (1) HRP20140950T1 (es)
HU (1) HUS1900009I1 (es)
IL (1) IL205974A (es)
LT (1) LTPA2019003I1 (es)
LU (1) LUC00103I2 (es)
MA (1) MA31936B1 (es)
ME (2) ME01294B (es)
MX (1) MX2010005776A (es)
MY (1) MY147370A (es)
NO (1) NO2016016I2 (es)
NZ (4) NZ601786A (es)
PL (1) PL2217577T3 (es)
PT (1) PT2217577E (es)
RS (1) RS53569B1 (es)
SG (1) SG183721A1 (es)
SI (1) SI2217577T1 (es)
TN (1) TN2010000237A1 (es)
TW (1) TWI415840B (es)
WO (1) WO2009070740A2 (es)
ZA (1) ZA201003769B (es)

Families Citing this family (99)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE528001T1 (de) * 2004-08-25 2011-10-15 Ardea Biosciences Inc S-triazolyl-alpha-mercaptoacetanilide als inhibitoren von hiv-umkehrtranskriptase
WO2007050087A1 (en) 2004-08-25 2007-05-03 Ardea Biosciences, Inc. N[S(4-aryl-triazol-3-yl)α -mercaptoacetyl]-p-amino benozoic acids AS HIV REVERSE TRANSCRIPTASE INHIBITORS
CN103058944B (zh) 2007-11-27 2015-08-05 亚德生化公司 调节血液尿酸水平的化合物
US8242154B2 (en) * 2008-09-04 2012-08-14 Ardea Biosciences, Inc. Compounds, compositions and methods of using same for modulating uric acid levels
KR101294872B1 (ko) * 2008-09-04 2013-08-08 아디아 바이오사이언스즈 인크. 요산 수치를 조절하기 위한 화합물, 조성물 및 이들의 사용 방법
US8173690B2 (en) 2008-09-04 2012-05-08 Ardea Biosciences, Inc. Compounds, compositions and methods of using same for modulating uric acid levels
EP2349258A1 (en) * 2008-10-24 2011-08-03 Ardea Biosciences, Inc. Compositions comprising 4- (2- ( 5-br0m0-4- ( l-cyclopropylnaphthalen-4-yl) -4h-1, 2, 4-triazol-3-ylthio) acetamido -3-chlorobenzoic acid and pharmaceutically acceptable salts thereof
WO2010048592A1 (en) * 2008-10-24 2010-04-29 Ardea Biosciences, Inc. Compositions comprising 4- (2- ( 5-br0m0-4- ( 1-cyclopropylnaphthalen-4-yl) -4h-1, 2, 4-triaz0l-3-ylthi0) acetamido -3-chlorobenzoic acid and pharmaceutically acceptable salts thereof
WO2010071865A1 (en) 2008-12-19 2010-06-24 Nuon Therapeutics, Inc. Pharmaceutical compositions and methods for treating hyperuricemia and related disorders
US20100160351A1 (en) * 2008-12-19 2010-06-24 Nuon Therapeutics, Inc. Pharmaceutical compositions and methods for treating hyperuricemia and related disorders
US8372807B2 (en) 2009-05-20 2013-02-12 Ardea Biosciences, Inc. Methods of modulating uric acid levels
EP2432774A4 (en) * 2009-05-20 2013-01-02 Ardea Biosciences Inc COMPOUNDS, COMPOSITIONS AND METHODS FOR MODULATING URIC ACID RATES
PH12012501391A1 (en) * 2010-01-08 2012-10-29 Ardea Biosciences Inc Polymorphic, crystalline and mesophase forms of sodium 2-(5-bromo-4-(4-cyclopropylnaphthalen-1-yl)-4h-1,2,4-triazol-3-ylthio)acetate, and uses thereof
CA2794798C (en) * 2010-03-30 2017-05-30 Ardea Biosciences, Inc. Treatment of gout
RS57275B1 (sr) * 2010-06-15 2018-08-31 Ardea Biosciences Inc Tretman gihta i hiperurikemije
JP5709146B2 (ja) * 2010-06-16 2015-04-30 アルデア バイオサイエンシーズ インク． フェニルチオ酢酸化合物、組成物、および、その使用方法
AR081930A1 (es) * 2010-06-16 2012-10-31 Ardea Biosciences Inc Compuestos de tioacetato
CA2813555C (en) * 2010-10-15 2014-11-25 Ardea Biosciences, Inc. Methods for treating hyperuricemia and related diseases
BR112013010270A2 (pt) * 2010-10-28 2016-07-05 Mapi Pharma Ltd polimorfos de febuxostato
EP2658846B1 (en) * 2010-12-30 2016-12-14 Ardea Biosciences, Inc. Polymorphic forms of 2-(5-bromo-4-(4-cyclopropylnaphthalen-1-yl)-4h-1,2,4-triazol-3-ylthio) acetic acid and uses thereof
WO2012122532A2 (en) * 2011-03-09 2012-09-13 Biocryst Pharmaceuticals, Inc. Compositions and methods for treatment of hyperuricemia
CA2837080C (en) * 2011-05-24 2017-01-24 Ardea Biosciences, Inc. Hypertension and hyperuricemia
EP2567959B1 (en) 2011-09-12 2014-04-16 Sanofi 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
SG11201402016PA (en) * 2011-11-03 2014-05-29 Ardea Biosciences Inc 3,4-di-substituted pyridine compound, methods of using and compositions comprising the same
US9023856B2 (en) 2011-11-04 2015-05-05 Cymabay Therapeutics, Inc. Methods for treating hyperuricemia in patients with gout using halofenate or halogenic acid and a second urate-lowering agent
SG11201401981TA (en) * 2011-11-04 2014-05-29 Metabolex Inc Methods for treating gout flares
US9060987B2 (en) 2011-11-04 2015-06-23 Cymabay Therapeutics, Inc. Methods for treating gout flares
BR112014010693A2 (pt) * 2011-11-04 2020-11-10 Cymabay Therapeutics, Inc. uso de um composto para a preparação de uma composição farmacêutica para o tratamento de gota em subpopulações de pacientes
HK1201209A1 (en) * 2012-01-27 2015-08-28 帝人制药株式会社 Therapeutic agent for diabetes
AR091651A1 (es) * 2012-07-03 2015-02-18 Ardea Biosciences Inc Elaboracion de acido 2-(5-bromo-4-(4-ciclopropilnaftalen-1-il)-4h-1,2,4-triazol-3-iltio)acetico
NO2944633T3 (es) * 2012-11-14 2018-06-30
CN102973530B (zh) * 2012-12-14 2016-08-03 贵州信邦制药股份有限公司 一种非布索坦双层肠溶片剂及其制备方法
EP2998296B1 (en) 2013-05-13 2018-03-14 Shanghai Hengrui Pharmaceutical Co. Ltd. Cycloalkyl acid derivative, preparation method thereof, and pharmaceutical application thereof
WO2014198241A1 (en) * 2013-06-14 2014-12-18 Sunshine Lake Pharma Co., Ltd. Thio-1,2,4-triazole derivatives and method for preparing the same
CN103524440B (zh) * 2013-10-15 2015-09-09 苏州鹏旭医药科技有限公司 痛风治疗药Lesinurad的制备方法及Lesinurad中间体
CN104447589B (zh) * 2013-11-20 2017-01-11 广东东阳光药业有限公司 一种尿酸调节剂的制备方法及其中间体
CN103613552A (zh) * 2013-12-02 2014-03-05 苏州晶云药物科技有限公司 2-(5-溴-4-(4-环丙基萘-1-基)-4h-1，2，4-三唑-3-基硫基)乙酸钠的新晶型及其制备方法
CN103588716A (zh) * 2013-11-22 2014-02-19 苏州晶云药物科技有限公司 2-(5-溴-4-(4-环丙基萘-1-基)-4h-1，2，4-三唑-3-基硫基)乙酸的新晶型及其制备方法
US10351536B2 (en) * 2013-11-22 2019-07-16 Crystal Pharmatech Co., Ltd. Crystalline forms of lesinurad and its sodium salt
CN103626710A (zh) * 2013-12-20 2014-03-12 苏州晶云药物科技有限公司 2-(5-溴-4-(4-环丙基萘-1-基)-4h-1，2，4-三唑-3-基硫基)乙酸的共晶及其制备方法
US9969701B2 (en) * 2013-12-20 2018-05-15 Crystal Pharmatech Co., Ltd. Salts and co-crystals of lesinurad
CN103755651A (zh) * 2013-12-23 2014-04-30 苏州晶云药物科技有限公司 2-(5-溴-4-(4-环丙基萘-1-基)-4h-1，2，4-三唑-3-基硫基)乙酸的盐的新晶型及其制备方法
CN105294585B (zh) * 2014-07-02 2019-02-12 成都海创药业有限公司 一种治疗痛风的化合物
CN104068288B (zh) * 2014-07-25 2016-08-24 许伟琦 一种防尿路结石的饲料添加剂
CN104326995A (zh) * 2014-10-27 2015-02-04 张远强 一种腈基取代的三氮唑丙二酸类化合物、其制备方法及用途
CN104326998B (zh) * 2014-10-27 2016-08-17 张远强 苯基取代的三氮唑丙二酸类化合物、其制备方法及用途
CN104326996A (zh) * 2014-10-27 2015-02-04 张远强 一种硝基取代三氮唑丙二酸类化合物、其制备方法及用途
CN104341362B (zh) * 2014-10-27 2016-07-13 张远强 三氮唑磺酰丙二酸类化合物、其制备方法及用途
CN104326993B (zh) * 2014-10-27 2016-08-17 张远强 一种硝基取代三氮唑亚磺酰丙二酸类化合物、其制备方法及用途
CN104370842B (zh) * 2014-10-27 2016-07-13 张远强 苯基取代的三氮唑磺酰丙二酸类化合物、其制备方法及用途
CN104327000B (zh) * 2014-10-27 2016-08-17 张远强 苯基取代的三氮唑亚磺酰丙二酸类化合物、其制备方法及用途
CN104341365A (zh) * 2014-10-27 2015-02-11 张远强 卤代三氮唑丙二酸类化合物、其制备方法及用途
CN104341364A (zh) * 2014-10-27 2015-02-11 张远强 三氮唑丙二酸类化合物、其制备方法及用途
CN104326994A (zh) * 2014-10-27 2015-02-04 张远强 一种腈基取代的三氮唑磺酰丙二酸类化合物、其制备方法及用途
CN104341363B (zh) * 2014-10-27 2016-08-17 张远强 一种硝基取代的三氮唑磺酰丙二酸类化合物、其制备方法及用途
CN104370841B (zh) * 2014-10-27 2016-07-13 张远强 三氮唑亚磺酰丙二酸类化合物、其制备方法及用途
CN104529848A (zh) * 2014-11-10 2015-04-22 安徽万邦医药科技有限公司 一种1-环丙基-4-异硫氰酰基萘的合成方法
WO2016105499A1 (en) 2014-12-23 2016-06-30 Intellectual Property Associates, Llc Methods and formulations for transdermal administration
KR102556608B1 (ko) 2014-12-29 2023-07-17 닛뽕 케미파 가부시키가이샤 Urat1 저해제
CN109053608A (zh) * 2015-02-17 2018-12-21 华润赛科药业有限责任公司 一种旋光纯的硫代乙酸类化合物、其药物组合物和用途
CN105622531A (zh) 2015-04-03 2016-06-01 南京明德新药研发股份有限公司 轴手性异构体及其制备方法和制药用途
CN104710374A (zh) * 2015-04-14 2015-06-17 安徽省逸欣铭医药科技有限公司 一种痛风新化合物及制备方法、用途及其药物制剂
CN106187926B (zh) 2015-04-30 2018-11-27 天津药物研究院有限公司 含二芳基甲烷结构的羧酸类urat1抑制剂、制备方法及其在高尿酸血症和痛风治疗上的用途
WO2016203436A1 (en) * 2015-06-19 2016-12-22 Dr. Reddy's Laboratories Limited Amorphous and amorphous solid dispersion of lesinurad and their preparation
EP3112334A1 (en) 2015-06-29 2017-01-04 DPx Fine Chemicals Austria GmbH & CoKG Process for manufacturing 1-cyclopropyl-naphthalenes
CN104987311A (zh) * 2015-06-30 2015-10-21 安徽万邦医药科技有限公司 一种[4-(4-环丙基萘-1-基)-5-硝基- 4h-[1,2,4]三唑-3-基硫烷基]-乙酸乙酯的制备方法及其中间体(5-硝基-4h-[1,2,4]三唑-3-基硫基)-乙酸乙酯
CN105153056A (zh) * 2015-07-01 2015-12-16 安徽万邦医药科技有限公司 一种[5-溴-4-(4-环丙基萘-1-基)-4h-[1,2,4]三唑-3-基硫烷基]-乙酸甲酯的新制备方法
CN105017168A (zh) * 2015-07-01 2015-11-04 安徽万邦医药科技有限公司 一种[5-溴-4-(4-环丙基萘-1-基)-4h-[1,2,4]三唑-3-基硫烷基]-乙酸甲酯的新制备方法
RU2728722C2 (ru) * 2015-08-26 2020-07-30 Стаджен Ко., Лтд. Усилитель внутриклеточного атф
WO2017036884A1 (en) 2015-08-28 2017-03-09 Sandoz Ag A lesinurad, free form / lesinurad ethyl ester co-crystal
CN105301126B (zh) * 2015-10-10 2021-02-12 大道隆达（北京）医药科技发展有限公司 一种托匹司他有关物质的分析方法
US10626096B2 (en) 2015-11-24 2020-04-21 Sanford Burnham Prebys Medical Discovery Institute Azole derivatives as apelin receptor agonist
US10894038B2 (en) 2015-12-28 2021-01-19 Shanghai Fochon Pharmaceutical Co. Ltd. Indolizine derivatives, composition and methods of use
WO2017147270A1 (en) * 2016-02-24 2017-08-31 Ardea Biosciences, Inc. Atropisomers of triazole derivative
CN107176930B (zh) * 2016-03-11 2020-12-01 广东赛烽医药科技有限公司 2-[5-溴-4-(4-氟代环丙基萘-1-基)-4h-1，2，4-三唑-3-基硫基]乙酸化合物及其应用
CN107337649B (zh) * 2016-04-29 2020-10-16 四川科伦药物研究院有限公司 一种乙酸钠水合物无定型及其制备方法和用途
CN109790155B (zh) 2016-05-23 2022-02-18 东宝紫星(杭州)生物医药有限公司 噻吩化合物及其合成方法和其在医药上的应用
CN106074540B (zh) * 2016-06-10 2018-10-16 江西博屾医疗器械有限公司 一种用于高尿酸血症治疗的药物组合物及其应用
CN109476611B (zh) * 2016-06-17 2022-08-23 南京明德新药研发有限公司 一种卤代化合物及其轴手性异构体
CN105943552A (zh) * 2016-06-17 2016-09-21 王枝宝 一种氢氧化钾的医药用途
CN106083847B (zh) * 2016-08-03 2018-10-30 山东大学 一种咪唑并吡啶巯乙酸类衍生物及其制备方法与应用
EP3281941B1 (en) 2016-08-11 2019-07-24 Zentiva K.S. Process for preparing 2-(5-bromo-4-(1-cyclopropylnaphthalen-4-yl)-4h-1,2,4-triazol-3-ylthio)acetic acid
CZ307277B6 (cs) * 2016-09-30 2018-05-09 Zentiva, K.S. Způsob výroby 2-(5-brom-4-(1-cyklopropylnaftalen-4-yl)-4H-1,2,4-triazol-3-ylthio)octové kyseliny - lesinuradu
CN108014108A (zh) * 2016-11-03 2018-05-11 江苏万邦生化医药股份有限公司 lesinurad或其医药上可接受的盐在制备治疗或预防库欣综合征的药物中的应用
CA3042738A1 (en) 2016-11-10 2018-05-17 Apotex Inc. Novel crystalline forms of lesinurad
CN110121359A (zh) 2016-11-11 2019-08-13 怀特黑德生物制剂研究所 人血浆培养基
CN108164471B (zh) * 2016-12-07 2019-09-13 浙江京新药业股份有限公司 Lesinurad衍生物及其制备方法和用途
US10351537B2 (en) 2017-03-10 2019-07-16 Apotex Inc. Processes for the preparation of lesinurad and intermediates thereof
EP3315494A1 (en) 2017-04-19 2018-05-02 Química Sintética, S.A. Amorphous form of lesinurad and processes for its preparation
CN108947919B (zh) * 2017-05-17 2023-05-02 上海奥博生物医药股份有限公司 一种抗痛风药Lesinurad的新型制备方法及其关键中间体
US10538808B2 (en) 2017-05-26 2020-01-21 Vibrant Holdings, Llc Photoactive compounds and methods for biomolecule detection and sequencing
WO2019055880A2 (en) 2017-09-15 2019-03-21 Ampersand Biopharmaceuticals, Inc. METHOD OF ADMINISTRATION AND TREATMENT
NZ765226A (en) 2017-11-23 2022-11-25 Medshine Discovery Inc Crystal form of urat1 inhibitor, and preparation method therefor
EP3498697A1 (en) 2017-12-12 2019-06-19 Química Sintética, S.A. Novel salts and polymorphs of lesinurad
KR102660247B1 (ko) * 2017-12-15 2024-04-25 지앙수 카니온 파마수티컬 씨오., 엘티디. 4-(나프탈렌-1-일)-4h-1, 2, 4-트리아졸계 화합물의 결정 형태, 염 형태 및 이의 제조방법
EP3790985A4 (en) 2018-05-09 2022-02-16 Vibrant Holdings, LLC METHOD OF SYNTHESIS OF A POLYNUCLEOTIDARRAY USING PHOTOACTIVATED AGENTS
MY204234A (en) 2018-08-27 2024-08-16 Regeneron Pharma Use of raman spectroscopy in downstream purification
CN109369783B (zh) * 2018-11-30 2021-09-10 昆明医科大学 一种多肽rdp1及其提纯方法与应用
CN111320588B (zh) * 2018-12-14 2024-02-09 上海奥博生物医药股份有限公司 一种纯化Lesinurad的方法

Family Cites Families (50)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2006101A (en) 1932-07-05 1935-06-25 Meaf Mach En Apparaten Fab Nv Reversing mechanism for dry gas meters
NL7112373A (es) * 1970-09-25 1972-03-28
US4198513A (en) * 1970-09-25 1980-04-15 Merck & Co., Inc. 1,2,4-Triazoles
JPS5641637B2 (es) 1973-11-26 1981-09-29
US4889868A (en) 1984-12-20 1989-12-26 Rorer Pharmaceutical Corporation Bis-imidazolinoamino derivatives as antiallergy compounds
US5260322A (en) * 1990-10-08 1993-11-09 Merck & Co., Inc. Angiotension II antagonists in the treatment of hyperuricemia
US6832996B2 (en) * 1995-06-07 2004-12-21 Arthrocare Corporation Electrosurgical systems and methods for treating tissue
JPH07215940A (ja) 1994-01-27 1995-08-15 Torii Yakuhin Kk 抗ウイルス活性を有する化合物
AU2395095A (en) 1994-04-29 1995-11-29 G.D. Searle & Co. Method of using (h+/k+) atpase inhibitors as antiviral agents
JP3964478B2 (ja) 1995-06-30 2007-08-22 エーザイ・アール・アンド・ディー・マネジメント株式会社 ヘテロ環含有カルボン酸誘導体及びそれを含有する医薬
US6017925A (en) 1997-01-17 2000-01-25 Merck & Co., Inc. Integrin antagonists
JP2000510164A (ja) * 1997-02-14 2000-08-08 バイエル・コーポレーシヨン 選択的神経ペプチドｙ受容体アンタゴニストとしてのアミド誘導体
US6245817B1 (en) * 1997-02-14 2001-06-12 Bayer Corporation NPY5 receptor antagonists and methods for using same
ES2361146T3 (es) * 1998-03-27 2011-06-14 Janssen Pharmaceutica Nv Derivados de la piramidina inhibitatoria de vih.
IL143105A0 (en) 1998-11-12 2002-04-21 Neurocrine Biosciences Inc Fused polycyclic heterocyclic compounds and pharmaceutical compositions containing the same
AU2217200A (en) * 1998-12-23 2000-07-12 Neurogen Corporation 2-amino-9-alkylpurines: gaba brain receptor ligands
US6593077B2 (en) * 1999-03-22 2003-07-15 Special Materials Research And Technology, Inc. Method of making thin films dielectrics using a process for room temperature wet chemical growth of SiO based oxides on a substrate
US6624194B1 (en) * 1999-06-04 2003-09-23 Metabolex, Inc. Use of (−) (3-trihalomethylphenoxy) (4-halophenyl) acetic acid derivatives for treatment of insulin resistance, type 2 diabetes, hyperlipidemia and hyperuricemia
PL364658A1 (en) 2001-03-02 2004-12-13 Smithkline Beecham Corporation Benzophenones as inhibitors of reverse transcriptase
JO3429B1 (ar) 2001-08-13 2019-10-20 Janssen Pharmaceutica Nv مشتقات برميدينات مثبطة فيروس الايدز
JP3600832B2 (ja) 2002-01-28 2004-12-15 株式会社富士薬品 新規１，２，４−トリアゾール系化合物
WO2003097047A1 (en) 2002-05-13 2003-11-27 Eli Lilly And Company Multicyclic compounds for use as melanin concentrating hormone antagonists in the treatment of obesity and diabetes
US20060135556A1 (en) * 2002-08-23 2006-06-22 Jean-Luc Girardet Non-nucleoside reverse transcriptase inhibitors
US7642277B2 (en) * 2002-12-04 2010-01-05 Boehringer Ingelheim International Gmbh Non-nucleoside reverse transcriptase inhibitors
KR20110132482A (ko) 2003-02-07 2011-12-07 얀센 파마슈티카 엔.브이. Ｈｉｖ 감염 예방용 피리미딘 유도체
KR20060121878A (ko) 2003-09-25 2006-11-29 얀센 파마슈티카 엔.브이. Ｈｉｖ를 저해하는 퓨린 유도체
US20080031901A1 (en) * 2004-09-24 2008-02-07 Abbott Laboratories Sustained release monoeximic formulations of opioid and nonopioid analgesics
US8236488B2 (en) 2003-11-14 2012-08-07 Human Cell Systems, Inc. Method of screening for therapeutic compounds for vascular disorders and hypertension based on URAT1 activity modulation
EP1694323A4 (en) 2003-12-19 2009-05-13 Elixir Pharmaceuticals Inc METHOD FOR TREATING A DISEASE
CN1934095A (zh) * 2004-03-08 2007-03-21 惠氏公司 离子通道调节剂
US20070203194A1 (en) 2004-03-08 2007-08-30 Scion Pharmaceuticals, Inc. Ion channel modulators
RU2006145872A (ru) 2004-05-25 2008-06-27 Метаболекс, Инк. (Us) Замещенные триазолы в качестве модуляторов ppar и способы их получения
US20060013556A1 (en) * 2004-07-01 2006-01-19 Thomas Poslinski Commercial information and guide
ATE528001T1 (de) * 2004-08-25 2011-10-15 Ardea Biosciences Inc S-triazolyl-alpha-mercaptoacetanilide als inhibitoren von hiv-umkehrtranskriptase
WO2007050087A1 (en) 2004-08-25 2007-05-03 Ardea Biosciences, Inc. N[S(4-aryl-triazol-3-yl)α -mercaptoacetyl]-p-amino benozoic acids AS HIV REVERSE TRANSCRIPTASE INHIBITORS
GB0422057D0 (en) 2004-10-05 2004-11-03 Astrazeneca Ab Novel compounds
WO2007043400A1 (ja) * 2005-10-07 2007-04-19 Kissei Pharmaceutical Co., Ltd. 含窒素芳香族複素環化合物およびそれを含有する医薬組成物
WO2007077042A1 (en) 2006-01-06 2007-07-12 Topotarget Switzerland Sa New method for the treatment of gout or pseudogout
EP2001897A2 (en) 2006-03-22 2008-12-17 Syndexa Pharmaceuticals Corporation Compounds and methods for treatment of disorders associated with er stress
CA2653217A1 (en) 2006-05-25 2007-12-06 Synta Pharmaceuticals Corp. Method for treating proliferative disorders associated with protooncogene products
EP2026797A2 (en) 2006-05-25 2009-02-25 Synta Pharmaceuticals Corporation Method for treating non-hodgkin's lymphoma
EP2061760A1 (en) 2006-09-07 2009-05-27 Amgen, Inc Benzo-fused compounds for use in treating metabolic disorders
EP1939181A1 (en) 2006-12-27 2008-07-02 sanofi-aventis Heteroaryl-substituted carboxamides and use thereof for the stimulation of the expression of NO synthase
MX2009007680A (es) 2007-01-19 2011-08-03 Takeda Pharmaceuticals North America Inc Metodos para prevenir o reducir el numero de expansiones graduales de gota utilizando inhibidores de oxidoreductasa de xantina y agentes anti-inflamatorios.
CN103058944B (zh) 2007-11-27 2015-08-05 亚德生化公司 调节血液尿酸水平的化合物
US8242154B2 (en) * 2008-09-04 2012-08-14 Ardea Biosciences, Inc. Compounds, compositions and methods of using same for modulating uric acid levels
US8173690B2 (en) 2008-09-04 2012-05-08 Ardea Biosciences, Inc. Compounds, compositions and methods of using same for modulating uric acid levels
WO2010048592A1 (en) 2008-10-24 2010-04-29 Ardea Biosciences, Inc. Compositions comprising 4- (2- ( 5-br0m0-4- ( 1-cyclopropylnaphthalen-4-yl) -4h-1, 2, 4-triaz0l-3-ylthi0) acetamido -3-chlorobenzoic acid and pharmaceutically acceptable salts thereof
WO2010071865A1 (en) 2008-12-19 2010-06-24 Nuon Therapeutics, Inc. Pharmaceutical compositions and methods for treating hyperuricemia and related disorders
CA2837080C (en) 2011-05-24 2017-01-24 Ardea Biosciences, Inc. Hypertension and hyperuricemia

Also Published As

Publication number Publication date
EA201270666A1 (ru) 2012-12-28
AU2008329673C1 (en) 2012-10-25
JP5905934B2 (ja) 2016-04-20
WO2009070740A2 (en) 2009-06-04
US8546437B2 (en) 2013-10-01
AU2012203172A1 (en) 2012-06-21
EP2217577B1 (en) 2014-08-06
RS53569B1 (sr) 2015-02-27
CN101918377A (zh) 2010-12-15
TW200927733A (en) 2009-07-01
ES2513390T3 (es) 2014-10-27
NZ585583A (en) 2011-09-30
DK2217577T3 (da) 2014-10-20
NO2016016I1 (no) 2016-08-17
US20090197825A1 (en) 2009-08-06
MY147370A (en) 2012-11-30
EA018193B3 (ru) 2014-07-30
MA31936B1 (fr) 2010-12-01
BRPI0819847B1 (pt) 2022-01-11
JP2014196373A (ja) 2014-10-16
NZ601786A (en) 2014-02-28
NZ595035A (en) 2012-11-30
CY2019010I2 (el) 2019-11-27
ME01996B (me) 2015-05-20
US8357713B2 (en) 2013-01-22
CA2706858A1 (en) 2009-06-04
AU2012203172B2 (en) 2013-10-10
BRPI0819847A2 (pt) 2020-10-06
ECSP10010310A (es) 2010-07-30
US8084483B2 (en) 2011-12-27
WO2009070740A3 (en) 2009-08-13
US20170281601A1 (en) 2017-10-05
SI2217577T1 (sl) 2014-11-28
US20110268801A1 (en) 2011-11-03
CA2706858C (en) 2013-12-24
HK1180337A1 (en) 2013-10-18
PT2217577E (pt) 2014-10-20
NZ601774A (en) 2013-07-26
KR101291643B1 (ko) 2013-08-01
EP2217577A2 (en) 2010-08-18
ME01294B (me) 2013-06-20
CL2008003529A1 (es) 2009-11-27
EP2842948A1 (en) 2015-03-04
CN103058944A (zh) 2013-04-24
EA201000897A1 (ru) 2010-12-30
JP2012184234A (ja) 2012-09-27
JP2011504935A (ja) 2011-02-17
US20160221970A1 (en) 2016-08-04
CN102643241B (zh) 2015-01-21
SG183721A1 (en) 2012-09-27
HUS1900009I1 (hu) 2019-03-28
IL205974A (en) 2015-03-31
MX2010005776A (es) 2010-08-31
US8283369B2 (en) 2012-10-09
AU2008329673A1 (en) 2009-06-04
US20190142805A1 (en) 2019-05-16
EA018193B1 (ru) 2013-06-28
TN2010000237A1 (en) 2011-11-11
LTPA2019003I1 (lt) 2019-02-25
TWI415840B (zh) 2013-11-21
HK1172326A1 (en) 2013-04-19
KR101411806B1 (ko) 2014-06-24
CN102643241A (zh) 2012-08-22
CN103058944B (zh) 2015-08-05
LUC00103I1 (es) 2019-02-19
US20140005136A1 (en) 2014-01-02
US20110293719A1 (en) 2011-12-01
EP2217577A4 (en) 2010-12-08
US10183012B2 (en) 2019-01-22
US20120164222A1 (en) 2012-06-28
IL205974A0 (en) 2010-11-30
AU2008329673B2 (en) 2012-04-12
LUC00103I2 (es) 2019-12-27
JP5099794B2 (ja) 2012-12-19
ZA201003769B (en) 2011-02-23
PL2217577T3 (pl) 2015-01-30
KR20120084787A (ko) 2012-07-30
NO2016016I2 (no) 2016-08-17
KR20100085195A (ko) 2010-07-28
CY2019010I1 (el) 2019-11-27
HRP20140950T1 (hr) 2014-12-05

Similar Documents

Publication Publication Date Title
AR069753A1 (es) Compuestos de 1,2,4-triazol y composiciones, utiles en la modulacion de los niveles de acido urico sanguineo
ES2477571T3 (es) Compuestos heterocíclicos como agentes antivirales
AR041009A1 (es) Compuestos heterociclicos nitrogenados que presentan actividad inhibitoria contra la integrasa del vih
ES2569399T3 (es) 2-(fenil o heterociclil)-1H-fenantro(9,10-d)imidazoles como inhibidores de la mPGES-1
CO5300399A1 (es) Heterocicliocs que contienen nitrogeno, proceso para su preparacion y composiciones farmaceuticas que los contienen
RU2006122209A (ru) Гетероароматические производные мочевины и их применение в качестве активаторов глюкокиназы
CO5150164A1 (es) Derivados de pirazolopiridina
AR070636A1 (es) Derivados de piridina, composicion farmaceutica y uso terapeutico
AR017177A1 (es) Compuesto derivados de 9-amino-3-ceto eritromicina, composiciones farmaceuticas, uso para la preparacion de un medicamento y procedimientos de preparacion.
HUP9702356A2 (hu) Glikogén foszforiláz inhibitor hatású 1H-indol-2-karbonsav-származékok alkalmazása gyógyászati készítmények előállítására
NO20083520L (no) Tricykliske N-heteroaryl-karboksamidderivater inneholdende en benzimidazolenhet, fremgangsmate for fremstilling av samme og deres terapeutiske anvendelser
PE20081577A1 (es) Derivados de sulfonamida ciclicos como inhibidores de la recaptacion de monoamina
AR035371A1 (es) Aminotiazoles, un metodo para su preparacion, composiciones farmaceuticas y el uso de dichos compuestos para la fabricacion de un medicamento
AR043049A1 (es) Derivados de hidantoina, proceso de preparacion del mismo y composicion farmaceutica
AR057855A1 (es) Derivados de pirazina y composicion farmaceutica
AR032453A1 (es) Derivados alquinil fenil heteroaromaticos activadores de glucoquinasa, un proceso para su preparacion, composiciones farmaceuticas, el uso de dichos derivados para la preparacion de medicamentos
RU2009113668A (ru) Производные аденозина как агонисты рецептора a2a
JP2007511535A5 (es)
AR063804A1 (es) Compuestos de azoniabiciclo[2.2.2]octano
AR087301A1 (es) Derivados de carboxamida y urea que contienen pirazol heteroaromatico sustituido como ligandos del receptor de vanilloide
AR041184A1 (es) Derivados de benzopiranonas, inhibidores de las cinasas dependientes de ciclinas y su uso
CR10034A (es) Derivados de oxadiazol
CY1116183T1 (el) Πιπεραζινοδιονες ως ανταγωνιστες υποδοχεα οξυτοκινης
ES2587304T3 (es) Derivados de diaminopirimidina y procedimientos para la preparación de los mismos
RU2001123126A (ru) Производные пиридопираноазепинов, их получение и терапевтическое применение

Legal Events

Date Code Title Description
FB Suspension of granting procedure