MXPA02006848A - Antagonistas del receptor de la hormona liberadora de gonadotropina. - Google Patents

Antagonistas del receptor de la hormona liberadora de gonadotropina.

Info

Publication number
MXPA02006848A
MXPA02006848A MXPA02006848A MXPA02006848A MXPA02006848A MX PA02006848 A MXPA02006848 A MX PA02006848A MX PA02006848 A MXPA02006848 A MX PA02006848A MX PA02006848 A MXPA02006848 A MX PA02006848A MX PA02006848 A MXPA02006848 A MX PA02006848A
Authority
MX
Mexico
Prior art keywords
protein
quantitating
image analysis
cells
optical density
Prior art date
Application number
MXPA02006848A
Other languages
English (en)
Inventor
Zhiqiang Guo
Original Assignee
Neurocrine Bioscience 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
Application filed by Neurocrine Bioscience Inc filed Critical Neurocrine Bioscience Inc
Publication of MXPA02006848A publication Critical patent/MXPA02006848A/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
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/60—Three or more oxygen or sulfur atoms
    • 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
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52—Two oxygen atoms
    • C07D239/54—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • 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
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61P15/18—Feminine contraceptives
    • 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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A61P5/02—Drugs for disorders of the endocrine system of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin
    • A61P5/04—Drugs for disorders of the endocrine system of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin for decreasing, blocking or antagonising the activity of the hypothalamic hormones
    • 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
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D401/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Urology & Nephrology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Anesthesiology (AREA)
  • Transplantation (AREA)
  • Pregnancy & Childbirth (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Investigating Or Analysing Biological Materials (AREA)

Abstract

Se describen antagonistas del receptor GnRH, los cuales tienen utilidad en el tratamiento de una variedad de condiciones relacionadas con la hormona sexual tanto en hombres como en mujeres. Los compuestos de la presente invencion tienen la estructura de la formula (1), en donde A, Q, R1, R2, R3a, R3b, R4, R5, R6 y n son tal como se define en la presente invencion, incluyendo estereoisomeros, profarmacos y sales farmaceuticamente aceptables de los mismos. Tambien se describen composiciones que contienen un compuesto de la presente invencion, en combinacion con un transportador farmaceuticamente aceptable, asi como metodos relacionados con el uso de los mismos para antagonizar la hormona de liberacion de gonadotropina en un sujeto que necesita de los mismos.
MXPA02006848A 2000-01-25 2001-01-25 Antagonistas del receptor de la hormona liberadora de gonadotropina. MXPA02006848A (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US17793300P 2000-01-25 2000-01-25
US23968300P 2000-10-11 2000-10-11
PCT/US2001/002740 WO2001055119A2 (en) 2000-01-25 2001-01-25 Gonadotropin-releasing hormone receptor antagonists and methods relating thereto

Publications (1)

Publication Number Publication Date
MXPA02006848A true MXPA02006848A (es) 2002-12-13

Family

ID=26873790

Family Applications (1)

Application Number Title Priority Date Filing Date
MXPA02006848A MXPA02006848A (es) 2000-01-25 2001-01-25 Antagonistas del receptor de la hormona liberadora de gonadotropina.

Country Status (15)

Country Link
US (4) US6608197B2 (es)
EP (1) EP1255738B1 (es)
JP (1) JP4931314B2 (es)
KR (1) KR100814269B1 (es)
AT (1) ATE548357T1 (es)
AU (1) AU767585B2 (es)
CA (1) CA2398018C (es)
CY (1) CY1112815T1 (es)
DK (1) DK1255738T3 (es)
ES (1) ES2383954T3 (es)
HK (1) HK1051042A1 (es)
MX (1) MXPA02006848A (es)
NO (1) NO20023525L (es)
PT (1) PT1255738E (es)
WO (1) WO2001055119A2 (es)

Families Citing this family (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MXPA02006848A (es) * 2000-01-25 2002-12-13 Neurocrine Bioscience Inc Antagonistas del receptor de la hormona liberadora de gonadotropina.
SE0100567D0 (sv) * 2001-02-20 2001-02-20 Astrazeneca Ab Compounds
US6939883B2 (en) 2001-08-02 2005-09-06 Neurocrine Biosciences, Inc. Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
EP1411941A2 (en) * 2001-08-02 2004-04-28 Neurocrine Biosciences, Inc. Pyridinone and pyridazinone derivatives as gonadotropin-releasing hormone receptor antagonists
WO2003086464A1 (fr) * 2002-04-12 2003-10-23 Takeda Pharmaceutical Company Limited. Agents pour prevenir/traiter les bouffees de chaleur
ATE428427T1 (de) * 2003-07-07 2009-05-15 Neurocrine Biosciences Inc Pyrimidin-2,4-dion-derivate als gonadotropin freisetzende hormon-rezeptor-antagonisten
US7015226B2 (en) * 2003-07-07 2006-03-21 Neurocrine Biosciences, Inc. Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
US7056927B2 (en) * 2003-07-07 2006-06-06 Neurocrine Biosciences, Inc. Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
CN102134230B (zh) * 2004-03-15 2019-06-28 武田药品工业株式会社 二肽基肽酶抑制剂
US20080262005A1 (en) * 2004-05-14 2008-10-23 Neurocrine Biosciences, Inc. Uracil-Type Gonadotropin-Releasing Hormone Receptor Antagonists and Methods Related Thereto
EP1655288A1 (en) * 2004-11-05 2006-05-10 Institut Pasteur Aryl pyrimidyl compounds, pharmaceutical compositions comprising them, their use as antimicrobial agents
SI1942898T2 (sl) 2005-09-14 2014-08-29 Takeda Pharmaceutical Company Limited Dipeptidil-peptidazni inhibitorji za zdravljenje diabetesa
CN102675221A (zh) * 2005-09-16 2012-09-19 武田药品工业株式会社 用于制备嘧啶二酮衍生物的方法中的中间体
WO2007122634A2 (en) * 2006-04-24 2007-11-01 Jubilant Biosys Limited Pyrimidinediones as tyrosine kinase inhibitors
TW200838536A (en) 2006-11-29 2008-10-01 Takeda Pharmaceutical Polymorphs of succinate salt of 2-[6-(3-amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethy]-4-fluor-benzonitrile and methods of use therefor
US8084614B2 (en) 2007-04-06 2011-12-27 Neurocrine Biosciences, Inc. Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
AR065947A1 (es) 2007-04-06 2009-07-15 Neurocrine Biosciences Inc Antagonistas de los receptores de la hormona liberadora de gonadodropina (gnrh)
US8426427B2 (en) * 2007-04-18 2013-04-23 Kissei Pharmaceutical Co., Ltd. Fused heterocyclic derivative, pharmaceutical composition comprising the derivative, and use of the composition for medical purposes
EP2145889A4 (en) * 2007-04-18 2012-04-18 Kissei Pharmaceutical HETEROCYCLIC FUSED CORE DERIVATIVE, PHARMACEUTICAL COMPOSITION COMPRISING THE DERIVATIVE, AND USE OF THE COMPOSITION FOR MEDICAL PURPOSES
WO2009062087A1 (en) * 2007-11-07 2009-05-14 Neurocrine Biosciences, Inc. Processes for the preparation of uracil derivatives
DE102008030091B4 (de) * 2008-06-25 2011-03-03 Resprotect Gmbh Uracilderivate und deren Verwendung
WO2010029299A1 (en) * 2008-09-12 2010-03-18 Biolipox Ab Pyrimidinone derivaties for use as medicaments
US9034850B2 (en) 2009-11-20 2015-05-19 Sk Chemicals Co., Ltd. Gonadotropin releasing hormone receptor antagonist, preparation method thereof and pharmaceutical composition comprising the same
TW201130854A (en) 2009-12-22 2011-09-16 Bayer Schering Pharma Ag Pyridinone derivatives and pharmaceutical compositions thereof
WO2012175514A1 (en) 2011-06-21 2012-12-27 Bayer Intellectual Property Gmbh Pyridinone derivatives and pharmaceutical compositions thereof
EP4223298A3 (en) 2013-03-15 2023-08-16 AbbVie Inc. Compositions for use in treating heavy menstrual bleeding
WO2018183923A1 (en) * 2017-03-31 2018-10-04 Epizyme, Inc. Methods of using ehmt2 inhibitors
EP3612181A4 (en) 2017-04-21 2021-01-06 Epizyme, Inc. COMBINATION THERAPIES WITH EHMT2 INHIBITORS
US20190054088A1 (en) 2017-08-18 2019-02-21 Abbvie Inc. Pharmaceutical Formulations for Treating Endometriosis, Uterine Fibroids, Polycystic Ovary Syndrome or Adenomyosis
WO2019203870A1 (en) 2018-04-19 2019-10-24 Abbvie Inc. Methods of treating heavy menstrual bleeding
WO2019036713A1 (en) 2017-08-18 2019-02-21 Abbvie Inc. SOLID PHARMACEUTICAL FORMULATIONS FOR THE TREATMENT OF ENDOMETRIOSIS, UTERINE FIBROIDS, POLYKYSTIC OVARY SYNDROME AND ADENOMYOSIS
CA3104902A1 (en) 2018-07-23 2020-01-30 Abbvie Inc. Elagolix sodium compositions and processes
EP3911327A4 (en) 2019-01-15 2022-10-26 Lupin Inc. DEUTERED ELAGOLIX-LIKE COMPOSITIONS AND PROCESSES
CN111333586A (zh) * 2020-02-19 2020-06-26 诚达药业股份有限公司 一种含有6-甲基尿嘧啶结构化合物的制备方法
CN111333587B (zh) * 2020-04-11 2023-04-07 东莞市东阳光新药研发有限公司 取代的嘧啶-2,4(1h,3h)-二酮衍生物及其用途
CN113527213B (zh) * 2020-04-20 2023-01-03 上海英诺富成生物科技有限公司 促性激素释放激素受体拮抗剂及其用途
CN117820248A (zh) * 2021-04-14 2024-04-05 盐野义制药株式会社 具有病毒增殖抑制作用的三嗪衍生物及含有其的药物组合物

Family Cites Families (36)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2631625B1 (fr) * 1988-05-17 1992-10-16 Synthelabo Derives de phenyl-6 piperazinylalkyl-3 1h,3h-pyrimidinedione-2,4, leur preparation et leur application en therapeutique
US5140029A (en) 1989-01-09 1992-08-18 Janssen Pharmaceutica N.V. 2-aminopyrimidinone derivatives
US5476855A (en) * 1993-11-02 1995-12-19 Mahmoud H. el Kouni Enzyme inhibitors, their synthesis and methods for use
UY23948A1 (es) * 1995-02-08 2001-10-25 Takeda Chemical Industries Ltd Derivados de anillos condensados de tiofeno su producción y uso.
CA2213510A1 (en) 1995-06-01 1996-12-05 Takeda Chemical Industries, Ltd. Diazepinones, their production and use
US5859014A (en) 1995-06-09 1999-01-12 Syntex (U.S.A.) Inc. Pyrimidinedione, pyrimidinetrione, triazinedione and tetrahydroquinazolinedione derivatives as α1 -adrenergic receptor antagonists
ATE201016T1 (de) * 1995-06-09 2001-05-15 Hoffmann La Roche Pyrimidindion-, pyrimidintrion-, triazindion- derivate als alpha-1-adrenergische rezeptorantagonisten
WO1997014697A1 (en) 1995-10-19 1997-04-24 Takeda Chemical Industries, Ltd. Thienopyridine derivatives as gonadotropin releasing hormone antagonists
ATE223902T1 (de) 1995-10-19 2002-09-15 Takeda Chemical Industries Ltd Chinolinderivate als gnrh antagonisten
US5849764A (en) 1995-12-14 1998-12-15 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
EA000992B1 (ru) 1995-12-14 2000-08-28 Мерк Энд Ко., Инк. Антагонисты гормона, высвобождающего гонадотропин
US5780437A (en) 1995-12-14 1998-07-14 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
US6197975B1 (en) 1995-12-14 2001-03-06 Merck & Co. , Inc. Antagonists of gonadotropin releasing hormone
AU704937B2 (en) 1995-12-14 1999-05-06 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
CZ183298A3 (cs) 1995-12-14 1998-09-16 Merck And Co., Inc. Nepeptidové deriváty, antagonizující hormon, uvolňující gonadotropin
JPH09286786A (ja) * 1996-04-18 1997-11-04 Nippon Paper Ind Co Ltd ピリミジン誘導体及びその抗腫瘍剤としての用途
EP0901471A4 (en) 1996-05-20 1999-08-25 Merck & Co Inc GONADOTROPIN RELEASING HORMONE ANTAGONISTS
JP2000511182A (ja) 1996-05-20 2000-08-29 メルク エンド カンパニー インコーポレーテッド 性腺刺激ホルモン放出ホルモンのアンタゴニスト
WO1997044339A1 (en) 1996-05-20 1997-11-27 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
WO1997044041A1 (en) 1996-05-20 1997-11-27 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
CA2291647A1 (en) 1997-06-05 1998-12-10 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
AU729752B2 (en) 1997-06-05 2001-02-08 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
AU7806998A (en) 1997-06-05 1998-12-21 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
JP2002502427A (ja) 1997-06-05 2002-01-22 メルク エンド カンパニー インコーポレーテッド ゴナドトロピン放出ホルモンの拮抗薬
US6313301B1 (en) 1997-08-13 2001-11-06 Takeda Chemical Industries, Ltd. Thienopyridine derivatives, their intermediates and production thereof
WO1999033831A1 (en) 1997-12-26 1999-07-08 Takeda Chemical Industries, Ltd. Nitrogen-containing heterocyclic compounds, their production and use
WO1999051232A1 (en) 1998-04-02 1999-10-14 Merck & Co., Inc. Antagonists of gonadotropin releasing hormone
WO2000029386A1 (en) * 1998-11-12 2000-05-25 Merck & Co., Inc. Pyrimidinedione derivatives useful as alpha 1a adrenoceptor antagonists
CA2372044A1 (en) 1999-05-14 2000-11-23 Neurocrine Biosciences, Inc. Imidazo- and pyrrolo[1,2-a]pyrimid-4-ones as gonadotropin-releasing hormone receptor antagonists
BR0011273A (pt) 1999-05-19 2002-06-18 Pharmacia Corp Uracilas de heteroarila e arila policìclica substituìdas como agentes anti-coagulantes
ES1043085Y (es) * 1999-06-03 2001-02-01 Nueva Ceramica Arb Sa Teja planoconvexa
JP2003512379A (ja) 1999-10-15 2003-04-02 ニューロクライン バイオサイエンシーズ， インコーポレイテッド 性腺刺激ホルモン放出ホルモンレセプターアンタゴニストおよびそれに関連する方法
MXPA02006848A (es) * 2000-01-25 2002-12-13 Neurocrine Bioscience Inc Antagonistas del receptor de la hormona liberadora de gonadotropina.
US7015226B2 (en) * 2003-07-07 2006-03-21 Neurocrine Biosciences, Inc. Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
US7056927B2 (en) * 2003-07-07 2006-06-06 Neurocrine Biosciences, Inc. Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
ATE428427T1 (de) * 2003-07-07 2009-05-15 Neurocrine Biosciences Inc Pyrimidin-2,4-dion-derivate als gonadotropin freisetzende hormon-rezeptor-antagonisten

Also Published As

Publication number Publication date
US7462625B2 (en) 2008-12-09
KR100814269B1 (ko) 2008-03-18
JP2003520856A (ja) 2003-07-08
CY1112815T1 (el) 2016-02-10
NO20023525D0 (no) 2002-07-24
US20070208049A1 (en) 2007-09-06
US7179815B2 (en) 2007-02-20
NO20023525L (no) 2002-07-24
EP1255738B1 (en) 2012-03-07
EP1255738A2 (en) 2002-11-13
US20040048884A1 (en) 2004-03-11
ATE548357T1 (de) 2012-03-15
AU767585B2 (en) 2003-11-20
US6608197B2 (en) 2003-08-19
US6872728B2 (en) 2005-03-29
CA2398018C (en) 2011-10-18
JP4931314B2 (ja) 2012-05-16
WO2001055119A3 (en) 2002-02-14
WO2001055119A2 (en) 2001-08-02
PT1255738E (pt) 2012-06-19
KR20030012846A (ko) 2003-02-12
AU3797501A (en) 2001-08-07
ES2383954T3 (es) 2012-06-27
CA2398018A1 (en) 2001-08-02
US20020132820A1 (en) 2002-09-19
US20050234082A1 (en) 2005-10-20
HK1051042A1 (en) 2003-07-18
DK1255738T3 (da) 2012-06-25

Similar Documents

Publication Publication Date Title
MXPA02006843A (es) Metodo para cuantificar una proteina por analisis de imagenes.
MXPA02006848A (es) Antagonistas del receptor de la hormona liberadora de gonadotropina.
RU2408735C2 (ru) Способ предсказания ответа на лечение
Hira et al. Comparison of different methodologies and cryostat versus paraffin sections for chromogenic immunohistochemistry
DK1774037T3 (da) Analyser og fremgangsmåder, der anvender biomarkører
ES2170220T3 (es) Procedimiento para detectar sustancias biologicamente activas.
EP0846949A4 (en) METHOD FOR DETECTING SOLID CANCER CELLS AND HISTOLOGICAL HETEROTYPES AND METHOD FOR TESTING TISSUE FOR BONE MARKET TRANSPLANTATION AND TRANSPLANTATION OF PERIPHERAL BLOOD STEM CELLS
Knabe et al. A method for immunohistochemical detection of osteogenic markers in undecalcified bone sections
ATE508205T1 (de) Tests und verfahren unter verwendung von biomarkern
ATE258310T1 (de) Testverfahren für collagenpeptid
Strack et al. Individual mitochondrion characterization: a comparison of classical assays to capillary electrophoresis with laser-induced fluorescence detection
Onuma et al. Quantitative analysis of the proliferation of epidermal cells using a human skin organ culture system and the effect of DbcAMP using markers of proliferation (BrdU, Ki-67, PCNA)
Hensbergen et al. Proteomic profiling identifies an UV-induced activation of cofilin-1 and destrin in human epidermis
Roussel et al. Quantification of Ag-NOR proteins using Ag-NOR staining on western blots.
DK0960336T3 (da) Peptidreagens til påvisning af humant cytomelagovirus (CMV)
DE60034966D1 (de) Auswertung von biologischen mitteln in lebenden zielzellen
ATE427494T1 (de) Verfahren zur quantifizierung der akt-protein- expression
Redpath High-resolution one-dimensional polyacrylamide gel isoelectric focusing of various forms of elongation factor-2
NZ595791A (en) High throughput assay systems and methods for identifying agents that alter expression of cellular proteins
Daniele et al. Pleomorphic adenoma and adenoid‐cystic carcinoma of salivary glands: immunohistochemical assessment of proliferative activity in comparison with flow‐cytometric study
NO983984L (no) Disintegrin-metalloprotease samt anvendelse derav
Zamolo et al. Expression of p53 and apoptosis in discoid lupus erythematosus.
Kimura et al. Detection of stimulants in hair by laser microscopy
Sarkaria et al. Squamous cell carcinoma–related oncogene is highly expressed in developing, normal, and adenomatous adrenal tissue but not in aggressive adrenocortical carcinomas
Zinellu et al. Protein‐bound glutathione measurement in cultured cells by CZE with LIF detection

Legal Events

Date Code Title Description
FG Grant or registration