WO2002098363A3 - NON-PEPTIDE GnRH AGENTS, PHARMACEUTICAL COMPOSITIONS AND METHODS FOR THEIR USES, AND PROCESSES FOR PREPARING THEM - Google Patents

NON-PEPTIDE GnRH AGENTS, PHARMACEUTICAL COMPOSITIONS AND METHODS FOR THEIR USES, AND PROCESSES FOR PREPARING THEM Download PDF

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Publication number
WO2002098363A3
WO2002098363A3 PCT/US2002/017846 US0217846W WO02098363A3 WO 2002098363 A3 WO2002098363 A3 WO 2002098363A3 US 0217846 W US0217846 W US 0217846W WO 02098363 A3 WO02098363 A3 WO 02098363A3
Authority
WO
WIPO (PCT)
Prior art keywords
methods
preparing
processes
pharmaceutical compositions
peptide gnrh
Prior art date
Application number
PCT/US2002/017846
Other languages
French (fr)
Other versions
WO2002098363A2 (en
Inventor
Eric T Sun
Mark B Anderson
Kenna L Anderes
Lance C Christie
Quyen-Quyen T Do
Jun Feng
Thomas Goetzen
Yufeng Hong
Eugenia A Iatsimirskaia
Haitao Li
David R Luthin
Genevieve D Paderes
Ved P Pathak
Ranjan Jagath Rajapakse
Scott Shackelford
Eileen Valenzuela Tompkins
Larry K Truesdale
Haresh VAZIR
Original Assignee
Agouron Pharma
Eric T Sun
Mark B Anderson
Kenna L Anderes
Lance C Christie
Quyen-Quyen T Do
Jun Feng
Thomas Goetzen
Yufeng Hong
Eugenia A Iatsimirskaia
Haitao Li
David R Luthin
Genevieve D Paderes
Ved P Pathak
Ranjan Jagath Rajapakse
Scott Shackelford
Eileen Valenzuela Tompkins
Larry K Truesdale
Haresh VAZIR
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 Agouron Pharma, Eric T Sun, Mark B Anderson, Kenna L Anderes, Lance C Christie, Quyen-Quyen T Do, Jun Feng, Thomas Goetzen, Yufeng Hong, Eugenia A Iatsimirskaia, Haitao Li, David R Luthin, Genevieve D Paderes, Ved P Pathak, Ranjan Jagath Rajapakse, Scott Shackelford, Eileen Valenzuela Tompkins, Larry K Truesdale, Haresh VAZIR filed Critical Agouron Pharma
Priority to CA002449843A priority Critical patent/CA2449843A1/en
Priority to BR0210191-2A priority patent/BR0210191A/en
Priority to MXPA03011002A priority patent/MXPA03011002A/en
Priority to EP02739712A priority patent/EP1401427A4/en
Priority to JP2003501405A priority patent/JP2005501006A/en
Priority to AU2002312348A priority patent/AU2002312348A1/en
Publication of WO2002098363A2 publication Critical patent/WO2002098363A2/en
Publication of WO2002098363A3 publication Critical patent/WO2002098363A3/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • 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
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • 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
    • 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
    • A61P5/02—Drugs for disorders of the endocrine system of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin
    • 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
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/56—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D307/68—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
    • C07D407/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Neurology (AREA)
  • Reproductive Health (AREA)
  • Communicable Diseases (AREA)
  • Immunology (AREA)
  • Biomedical Technology (AREA)
  • Oncology (AREA)
  • Neurosurgery (AREA)
  • Virology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Furan Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are described. Such compounds and their pharmaceutically acceptable salts, prodrugs, and active metabolites are suitable for treating mammalian reproductive disorders and steroid hormone-dependent tumors as well as for regulating fertility, where suppression of gonadotropin release is indicated. Methods for synthesizing the compounds and intermediates useful in their preparation are also described.
PCT/US2002/017846 2001-06-06 2002-06-05 NON-PEPTIDE GnRH AGENTS, PHARMACEUTICAL COMPOSITIONS AND METHODS FOR THEIR USES, AND PROCESSES FOR PREPARING THEM WO2002098363A2 (en)

Priority Applications (6)

Application Number Priority Date Filing Date Title
CA002449843A CA2449843A1 (en) 2001-06-06 2002-06-05 Non-peptide gnrh agents, pharmaceutical compositions and methods for their use, and processes for preparing them
BR0210191-2A BR0210191A (en) 2001-06-06 2002-06-05 Non-peptide Gnrh Agents, Pharmaceutical Compositions and Methods of Use, and Processes for Preparing them and Their Intermediates
MXPA03011002A MXPA03011002A (en) 2001-06-06 2002-06-05 NON-PEPTIDE GnRH AGENTS, PHARMACEUTICAL COMPOSITIONS AND METHODS FOR THEIR USES, AND PROCESSES FOR PREPARING THEM.
EP02739712A EP1401427A4 (en) 2001-06-06 2002-06-05 Non-peptide gnrh agents, pharmaceutical compositions and methods for their uses, and processes for preparing them
JP2003501405A JP2005501006A (en) 2001-06-06 2002-06-05 Non-peptide GnRH drugs, pharmaceutical compositions, uses thereof, methods for preparing these substances and intermediates thereof
AU2002312348A AU2002312348A1 (en) 2001-06-06 2002-06-05 Non-peptide gnrh agents, pharmaceutical compositions and methods for their uses, and processes for preparing them

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US29581201P 2001-06-06 2001-06-06
US60/295,812 2001-06-06
US30186801P 2001-06-29 2001-06-29
US60/301,868 2001-06-29

Publications (2)

Publication Number Publication Date
WO2002098363A2 WO2002098363A2 (en) 2002-12-12
WO2002098363A3 true WO2002098363A3 (en) 2003-03-20

Family

ID=26969346

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2002/017846 WO2002098363A2 (en) 2001-06-06 2002-06-05 NON-PEPTIDE GnRH AGENTS, PHARMACEUTICAL COMPOSITIONS AND METHODS FOR THEIR USES, AND PROCESSES FOR PREPARING THEM

Country Status (7)

Country Link
EP (1) EP1401427A4 (en)
JP (1) JP2005501006A (en)
AU (1) AU2002312348A1 (en)
BR (1) BR0210191A (en)
CA (1) CA2449843A1 (en)
MX (1) MXPA03011002A (en)
WO (1) WO2002098363A2 (en)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0130341D0 (en) * 2001-12-19 2002-02-06 Smithkline Beecham Plc Compounds
US7205307B2 (en) * 2002-02-14 2007-04-17 Icagen, Inc. Pyrimidines as novel openers of potassium ion channels
BR0312123A (en) 2002-06-13 2005-03-29 Pfizer Nonpeptide Gnrh Agents, Pharmaceutical Compositions and Methods for Their Use
US7332521B2 (en) * 2003-09-25 2008-02-19 Wyeth Substituted indoles
EP1541549A1 (en) * 2003-12-12 2005-06-15 Exonhit Therapeutics S.A. Tricyclic hydroxamate and benzaminde derivatives, compositions and methods
AU2007296743B2 (en) * 2006-09-11 2012-02-16 Curis, Inc. Tyrosine kinase inhibitors containing a zinc binding moiety
UA103319C2 (en) 2008-05-06 2013-10-10 Глаксосмитклайн Ллк Thiazole- and oxazole-benzene sulfonamide compounds
CN102329234B (en) * 2011-06-24 2013-11-06 灌南伊斯特化工有限公司 Production process of m-nitrobenzaldehyde
EP2712862A1 (en) * 2012-09-28 2014-04-02 Splicos New anti-invasive compounds
WO2014184682A1 (en) * 2013-04-19 2014-11-20 Oslo Universitetssykehus Hf Radiolabeled gnrh antagonists as pet imaging agents
CN108905641B (en) * 2018-08-01 2020-04-28 湖南七纬科技有限公司 Nanofiltration membrane and preparation method thereof
CN114105775A (en) * 2021-11-30 2022-03-01 武汉工程大学 Preparation method of substituted iodobenzene with terminal double bond

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6348480B1 (en) * 1997-10-13 2002-02-19 Yamanouchi Pharmaceutical Co., Ltd. Pharmaceutical compound comprising a pyrazole derivative and methods of using the same for the treatment of calcium release-activated calcium channel associated diseases

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR9908619A (en) * 1998-03-05 2001-10-02 Agouron Pharma Compound and its production process, pharmaceutical composition, and method to regulate the secretion of gonadotropins in mammals
ES2237966T3 (en) * 1998-08-20 2005-08-01 Agouron Pharmaceuticals, Inc. NON-PEPTIDIC AGENTS, METHODS AND INTERMEDIATE COMPOUNDS FOR PREPARATION.

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6348480B1 (en) * 1997-10-13 2002-02-19 Yamanouchi Pharmaceutical Co., Ltd. Pharmaceutical compound comprising a pyrazole derivative and methods of using the same for the treatment of calcium release-activated calcium channel associated diseases

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See also references of EP1401427A4 *

Also Published As

Publication number Publication date
JP2005501006A (en) 2005-01-13
AU2002312348A1 (en) 2002-12-16
BR0210191A (en) 2004-04-06
CA2449843A1 (en) 2002-12-12
EP1401427A2 (en) 2004-03-31
EP1401427A4 (en) 2004-12-01
MXPA03011002A (en) 2004-10-28
WO2002098363A2 (en) 2002-12-12

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