WO2000066564A8 - Benzimidazolones and analogues and their use as progesterone receptor ligands - Google Patents

Benzimidazolones and analogues and their use as progesterone receptor ligands

Info

Publication number
WO2000066564A8
WO2000066564A8 PCT/US2000/011824 US0011824W WO0066564A8 WO 2000066564 A8 WO2000066564 A8 WO 2000066564A8 US 0011824 W US0011824 W US 0011824W WO 0066564 A8 WO0066564 A8 WO 0066564A8
Authority
WO
WIPO (PCT)
Prior art keywords
alkyl
substituted
progesterone receptor
alkenyl
alkynyl
Prior art date
Application number
PCT/US2000/011824
Other languages
French (fr)
Other versions
WO2000066564A1 (en
Inventor
Puwen Zhang
Reinhold H W Bender
Lin Zhi
Todd K Jones
Christopher M Tegley
Jay E Wrobel
James P Edwards
Original Assignee
American Home Prod
Ligand Pharm Inc
Puwen Zhang
Reinhold H W Bender
Lin Zhi
Todd K Jones
Christopher M Tegley
Jay E Wrobel
James P Edwards
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 American Home Prod, Ligand Pharm Inc, Puwen Zhang, Reinhold H W Bender, Lin Zhi, Todd K Jones, Christopher M Tegley, Jay E Wrobel, James P Edwards filed Critical American Home Prod
Priority to EP00928690A priority Critical patent/EP1173423A1/en
Priority to JP2000615595A priority patent/JP2003517459A/en
Priority to CA002366805A priority patent/CA2366805A1/en
Priority to AU46887/00A priority patent/AU4688700A/en
Priority to MXPA01011290A priority patent/MXPA01011290A/en
Publication of WO2000066564A1 publication Critical patent/WO2000066564A1/en
Publication of WO2000066564A8 publication Critical patent/WO2000066564A8/en
Priority to HK02104863.4A priority patent/HK1043790A1/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/52—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
    • C07D263/54—Benzoxazoles; Hydrogenated benzoxazoles
    • C07D263/58—Benzoxazoles; Hydrogenated benzoxazoles 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
    • 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
    • A61P35/00—Antineoplastic agents
    • 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
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
    • C07C215/74—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton
    • C07C215/76—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton of the same non-condensed six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/02—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C229/04—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C229/06—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton
    • C07C229/18—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to carbon atoms of six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
    • C07D235/26—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/36—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems
    • C07D241/38—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems with only hydrogen or carbon atoms directly attached to the ring nitrogen atoms
    • C07D241/40—Benzopyrazines
    • C07D241/44—Benzopyrazines 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 carbon atoms of the hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62—Benzothiazoles
    • C07D277/68—Benzothiazoles 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D279/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
    • C07D279/10—1,4-Thiazines; Hydrogenated 1,4-thiazines
    • C07D279/14—1,4-Thiazines; Hydrogenated 1,4-thiazines condensed with carbocyclic rings or ring systems
    • C07D279/16—1,4-Thiazines; Hydrogenated 1,4-thiazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • 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
    • 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

Abstract

The present invention provides compounds and pharmaceutical formulations useful as progesterone receptor agonists and antagonists and having general formula (a): wherein A is O, S, or NR4; B is a bond between A and C=Q, or the moiety CR?5R6; R4, R5, R6¿ are independently selected from H or optionally substituted C¿1? to C6 alkyl, C2 to C6 alkenyl, C2 to C6 alkynyl, C3 to C8 cycloalkyl, substituted C3 to C8 cycloalkyl, aryl, or heteorcyclic groups, or cyclic alkyl constructed by fusing R?4 and R5¿ to from a 5 to 7 membered ring; R1 is selected from H, OH, NH¿2?, C1 to C6 alkyl, substituted C1 to C6 alkyl, C3 to C6 alkenyl, substituded C1 to C6 alkenyl, alkynyl, substituted alkynyl, -COH, or optionally substituted -CO(C1 to C3 alkyl), -CO(aryl), -CO(C1 to C3 alkoxy), or -CO(C1 toC3 aminoalkyl) groups; R?2¿ is selected from H, halogen, CN, NO¿2?, or optionally substituted C1 to C6 alkyl, C1 to C6 alkoxy, or C1 to C6 aminoalkyl groups; R?3¿ is selected from a trisubstituted benzene ring; or a 5- or 6- membered heteroaromatic ring containing 1 or 2 substituents; Q is O, S, NR?8, or CR9R10¿; or a pharmaceutically acceptable salt thereof. The invention also includes methods of contraception and methods of treating or preventing maladies associated with the progesterone receptor.
PCT/US2000/011824 1999-05-04 2000-05-01 Benzimidazolones and analogues and their use as progesterone receptor ligands WO2000066564A1 (en)

Priority Applications (6)

Application Number Priority Date Filing Date Title
EP00928690A EP1173423A1 (en) 1999-05-04 2000-05-01 Benzimidazolones and analogues and their use as progesterone receptor ligands
JP2000615595A JP2003517459A (en) 1999-05-04 2000-05-01 Benzimidazolones and analogs and their use as progesterone receptor ligands
CA002366805A CA2366805A1 (en) 1999-05-04 2000-05-01 Benzimidazolones and analogues and their use as progesterone receptor ligands
AU46887/00A AU4688700A (en) 1999-05-04 2000-05-01 Benzimidazolones and analogues and their use as progesterone receptor ligands
MXPA01011290A MXPA01011290A (en) 1999-05-04 2000-05-01 Benzimidazolones and analogues and their use as progesterone receptor ligands.
HK02104863.4A HK1043790A1 (en) 1999-05-04 2002-06-28 Benzimidazolones and analogues and their use as progesterone receptor ligands

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US18303699P 1999-05-04 1999-05-04
US60/183,036 1999-05-04
US09/552,546 2000-04-19
US09/552,546 US6380235B1 (en) 1999-05-04 2000-04-19 Benzimidazolones and analogues

Publications (2)

Publication Number Publication Date
WO2000066564A1 WO2000066564A1 (en) 2000-11-09
WO2000066564A8 true WO2000066564A8 (en) 2001-08-02

Family

ID=26878682

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2000/011824 WO2000066564A1 (en) 1999-05-04 2000-05-01 Benzimidazolones and analogues and their use as progesterone receptor ligands

Country Status (6)

Country Link
US (2) US6380235B1 (en)
EP (1) EP1173423A1 (en)
JP (1) JP2003517459A (en)
CN (1) CN1152020C (en)
CA (1) CA2366805A1 (en)
WO (1) WO2000066564A1 (en)

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CA2366805A1 (en) 2000-11-09
US6380235B1 (en) 2002-04-30
CN1349511A (en) 2002-05-15
EP1173423A1 (en) 2002-01-23
JP2003517459A (en) 2003-05-27
CN1152020C (en) 2004-06-02
US20020115853A1 (en) 2002-08-22
WO2000066564A1 (en) 2000-11-09

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