[go: up one dir, main page]

PE20061316A1 - Derivados de pirazol como antagonistas del receptor de progesterona - Google Patents

Derivados de pirazol como antagonistas del receptor de progesterona

Info

Publication number
PE20061316A1
PE20061316A1 PE2006000409A PE2006000409A PE20061316A1 PE 20061316 A1 PE20061316 A1 PE 20061316A1 PE 2006000409 A PE2006000409 A PE 2006000409A PE 2006000409 A PE2006000409 A PE 2006000409A PE 20061316 A1 PE20061316 A1 PE 20061316A1
Authority
PE
Peru
Prior art keywords
alkyl
receptor antagonists
progesterone receptor
oxy
halo
Prior art date
Application number
PE2006000409A
Other languages
English (en)
Inventor
Paul Anthony Bradley
Kevin Neil Dack
Ian Roger Marsh
Original Assignee
Pfizer Ltd
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 Pfizer Ltd filed Critical Pfizer Ltd
Publication of PE20061316A1 publication Critical patent/PE20061316A1/es

Links

Classifications

    • 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
    • C07D231/14—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 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
    • C07D231/28—Two oxygen or sulfur 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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/02—Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
    • 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
    • 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
    • C07D231/14—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 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
    • C07D231/18—One oxygen or sulfur atom
    • 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
    • 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
    • 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
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

SE REFIERE A UN COMPUESTO DE FORMULA I, DONDE R1 ES H, ALQUILO C1-C6, (ALQUILO C1-C6)-OXI, CICLOALQUILO C3-C8, HALO; R2 ES H, ALQUILO C1-C6 (SUSTITUIDO O NO CON R3), FENILO, HETEROARILO, ENTRE OTROS; R3 ES OH, CN, HETEROARILO, ENTRE OTROS; R8 ES ALQUILO C1-C6, CICLOALQUILO C3-C8, HALO, ENTRE OTROS; R9 Y R10 SON CADA UNO ALQUILO C1-C6, CF3, CN, HALO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 4-{[3,5-DICICLOPROPIL-1-(2-HIDROXIETIL)-1H-PIRAZOL-4-IL]OXI}-2,6-DIMETILBENZONITRILO; 4-{[1-(CIANOMETIL)-3,5-DIETIL-1H-PIRAZOL-4-IL]OXI}BENZONITRILO; 2-[4-(4-CIANOFENOXI)-3,5-DICICLOPROPIL-1H-PIRAZOL-1-IL]-N-METIL-ACETAMIDA; ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA Y A UN PROCEDIMIENTO DE PREPARACION. DICHOS COMPUESTOS SON ANTAGONISTAS DEL RECEPTOR DE PROGESTERONA UTILES EN EL TRATAMIENTO DE ENDOMETROSIS Y/O FIBROIDES UTERINOS
PE2006000409A 2005-04-20 2006-04-19 Derivados de pirazol como antagonistas del receptor de progesterona PE20061316A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US67354405P 2005-04-20 2005-04-20

Publications (1)

Publication Number Publication Date
PE20061316A1 true PE20061316A1 (es) 2007-01-13

Family

ID=35044974

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2006000409A PE20061316A1 (es) 2005-04-20 2006-04-19 Derivados de pirazol como antagonistas del receptor de progesterona

Country Status (12)

Country Link
US (2) US7482375B2 (es)
EP (1) EP1874732A1 (es)
JP (1) JP2008536910A (es)
AR (1) AR053587A1 (es)
CA (1) CA2604218A1 (es)
DO (1) DOP2006000088A (es)
GT (1) GT200600155A (es)
NL (1) NL1031626C2 (es)
PE (1) PE20061316A1 (es)
TW (1) TW200716609A (es)
UY (1) UY29486A1 (es)
WO (1) WO2006111856A1 (es)

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU714980B2 (en) 1996-07-24 2000-01-13 Warner-Lambert Company Llc Isobutylgaba and its derivatives for the treatment of pain
WO2008019048A1 (en) * 2006-08-04 2008-02-14 Meditrina Pharmaceuticals Use of aromatase inhibitors for thining the endometrium or treating menorrhagia
US20080096950A1 (en) * 2006-10-19 2008-04-24 Karl Richard Gibson Compounds Useful In Therapy
PE20081803A1 (es) * 2007-03-09 2008-12-11 Wyeth Corp Sintesis y caracterizacion de la forma ii polimorfica de 4-(2-(4,4-dimetil-2-oxooxazolidin-3-il)tiazol-4-il)benzonitrilo
WO2008135824A1 (en) * 2007-05-02 2008-11-13 Pfizer Limited Oxyalkylpyrazole compounds useful in therapy
WO2009075838A2 (en) * 2007-12-10 2009-06-18 Meditrina Pharmaceuticals, Inc. Treatment of menorrhagia with aromatase inhibitor
WO2009119880A1 (en) * 2008-03-26 2009-10-01 Takeda Pharmaceutical Company Limited Substituted pyrazole derivatives and use thereof
EP2116618A1 (en) 2008-05-09 2009-11-11 Agency for Science, Technology And Research Diagnosis and treatment of Kawasaki disease
EP2350017A1 (en) * 2008-09-18 2011-08-03 Pfizer Limited Amide compounds useful in therapy
US20150272622A1 (en) 2011-12-22 2015-10-01 Previvo Genetics, Llc Recovery and processing of human embryos formed in vivo
IN2014DN10548A (es) 2012-05-31 2015-08-21 Repros Therapeutics Inc
AU2013338305B2 (en) 2012-11-02 2018-06-07 Allergan pharmaceuticals International Ltd. Methods and compositions for treating progesterone-dependent conditions
EP2929883A1 (en) 2014-04-08 2015-10-14 Institut Pasteur Pyrazole derivatives as dihydroorotate dehydrogenase (DHODH) inhibitors
WO2015171392A1 (en) * 2014-05-06 2015-11-12 E. I. Du Pont De Nemours And Company Fungicidal pyrazoles
MX391191B (es) 2014-11-17 2025-03-21 Context Biopharma Inc Composiciones de liberación extendida de onapristona y métodos.
JP2018528944A (ja) 2015-09-25 2018-10-04 コンテクスト バイオファーマ インコーポレイテッド オナプリストン中間体の製造方法
JP2019503353A (ja) * 2015-12-15 2019-02-07 コンテキスト・バイオファーマ・インコーポレイテッド 非晶質オナプリストン組成物およびそれを作製する方法
WO2018102369A1 (en) 2016-11-30 2018-06-07 Arno Therapeutics, Inc. Methods for onapristone synthesis dehydration and deprotection
US20230414492A1 (en) * 2019-04-02 2023-12-28 Nose To Brain Therapeutics Llc Intranasal delivery of cannabidiol to treat central nervous system disorders

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3621024C2 (de) * 1986-06-20 1999-10-28 Schering Ag 11beta-Phenylestradiene, deren Herstellung und diese enthaltende pharmazeutische Präparate
DK1377556T3 (da) * 2001-04-10 2007-07-16 Pfizer Pyrazolderivater til behandling af HIV
US6933312B2 (en) * 2002-10-07 2005-08-23 Agouron Pharmaceuticals, Inc. Pyrazole derivatives

Also Published As

Publication number Publication date
EP1874732A1 (en) 2008-01-09
US20090099209A1 (en) 2009-04-16
DOP2006000088A (es) 2006-10-31
GT200600155A (es) 2007-04-18
NL1031626A1 (nl) 2006-10-23
JP2008536910A (ja) 2008-09-11
NL1031626C2 (nl) 2007-03-19
AR053587A1 (es) 2007-05-09
CA2604218A1 (en) 2006-10-26
UY29486A1 (es) 2006-11-30
US7482375B2 (en) 2009-01-27
WO2006111856A1 (en) 2006-10-26
US20060241125A1 (en) 2006-10-26
TW200716609A (en) 2007-05-01

Similar Documents

Publication Publication Date Title
PE20061316A1 (es) Derivados de pirazol como antagonistas del receptor de progesterona
PE20090772A1 (es) Derivados de bencimidazol
PE20070218A1 (es) COMPUESTOS DE CICLOALQUILO AMINO-HIDANTOINA Y USO DE ESTOS PARA LA MODULACION DE ß-SECRETASA
NO20063470L (no) Tetrazolforbindelser og deres anvendelse av metabotrofe glutamatreseptorantagonister
PE20071095A1 (es) Derivados policiclicos de indazol como inhibidores de erk
AR044874A1 (es) Derivados de 4- cianopirazol-3 - carboxamida, su preparacion y su aplicacion en terapeutica
PE20090601A1 (es) Derivados de piridin-il-oxi-piridinas como inhibidores de alk5
AR072952A1 (es) Compuestos de 2-imino-3-metilpirrolopirimidinona fenilo-sustituida como inhibidores de bace-1, composiciones y su uso
PE20091573A1 (es) Derivados heterociclicos de urea como inhibidores de adn girasa y/o topoisomerasa
PE20091974A1 (es) Derivados de indazoles sustituidos con fenil o piridinilo
PE20120635A1 (es) Dihidropirazolonas sustituidas como inhibidores de hif-propil-4-hidroxilasas
PE20061353A1 (es) Compuestos de sulfonamida-tiazolopiridina como activadores de glucocinasa
PE20140609A1 (es) Diazacarbazoles y metodos de uso
AR046085A1 (es) Agonistas etilamino amino sustituidos del receptor beta 2 adrenergico
PE20080318A1 (es) Derivados de diceto-piperazina y piperidina como agentes antivirales
PE20091033A1 (es) Derivados de nicotinamida como agentes anticancerosos y su preparacion
PE20070108A1 (es) Control de parasitos en animales con derivados de n-[(feniloxi)fenil]-1,1,1-trifluorometansulfonamida y de n-[(fenilsulfanil)fenil]-1,1,1-trifluorometansulfonamida
PE20081845A1 (es) Nuevos derivados de aminopirimidina como inhibidores de plk1
PE20120360A1 (es) Compuestos en calidad de antagonistas de bradiquinina b1
PE20030440A1 (es) Fenilsulfonamidas como antagonistas de ccr3
CR8505A (es) Derivados de (3-oxo-3,4-dihidroquinoxalin-2-il-amino)-benzamida y compuesto relacionado, como inhibidores de glucogeno fosforilasa para el tratamiento de la diabetes y obesidad
PE20090422A1 (es) Derivados de piperidina, piperazina o tetrahidropiridilo como antagonistas de trpv1
BRPI0608732A2 (pt) composto ou um sal, hidrato, solvato, complexo ou pró-droga farmaceuticamente aceitável do mesmo, sal de um composto, processo para a preparação de um composto, uso de um composto, composição farmacêutica, e, produto
PE20090620A1 (es) Derivados de 1,2,4,5-tetrahidro-3h-benzazepinas, su procedimiento de preparacion y las composiciones farmaceuticas que las contienen
PE20070833A1 (es) Compuestos de pirimidinil benzotiofeno

Legal Events

Date Code Title Description
FC Refusal