AR040783A1 - 5-(1',1'-cicloaquil/alquenil) metiliden-1,2 -dihidro-5-h-cromeno [3,4- f] quiinolinas como compuestos moduladores selectivos de receptores de progesterona - Google Patents

5-(1',1'-cicloaquil/alquenil) metiliden-1,2 -dihidro-5-h-cromeno [3,4- f] quiinolinas como compuestos moduladores selectivos de receptores de progesterona

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Publication number
AR040783A1
AR040783A1 AR20030102796A ARP030102796A AR040783A1 AR 040783 A1 AR040783 A1 AR 040783A1 AR 20030102796 A AR20030102796 A AR 20030102796A AR P030102796 A ARP030102796 A AR P030102796A AR 040783 A1 AR040783 A1 AR 040783A1
Authority
AR
Argentina
Prior art keywords
group
haloalkyl
alkyl
hydrogen
heteroalkyl
Prior art date
Application number
AR20030102796A
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English (en)
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Ligand Pharm 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 Ligand Pharm Inc filed Critical Ligand Pharm Inc
Publication of AR040783A1 publication Critical patent/AR040783A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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
    • C07D491/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/30Oestrogens
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/34Gestagens
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/74Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving hormones or other non-cytokine intercellular protein regulatory factors such as growth factors, including receptors to hormones and growth factors
    • G01N33/743Steroid hormones

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Molecular Biology (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Biomedical Technology (AREA)
  • Immunology (AREA)
  • Reproductive Health (AREA)
  • Food Science & Technology (AREA)
  • Analytical Chemistry (AREA)
  • Biotechnology (AREA)
  • Microbiology (AREA)
  • Diabetes (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physics & Mathematics (AREA)
  • Cell Biology (AREA)
  • Biochemistry (AREA)
  • General Physics & Mathematics (AREA)
  • Pathology (AREA)
  • Rheumatology (AREA)
  • Pregnancy & Childbirth (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

La presente se refiere a compuestos, composiciones farmacéuticas y métodos para modular procesos mediados por el receptor de la progesterona. También se proveen métodos para preparar tales compuestos y composiciones farmacéuticas. Reivindicación 1: Un compuesto de la fórmula (1) donde: R1 está seleccionado del grupo integrado por hidrógeno, alquilo C1-4, haloalquilo C1-4, heteroalquilo C1-4, COR5, CO2R5, SO2R5, y CONR5R6; R2 y R3 está seleccionados cada uno, de modo independiente, del grupo integrado por hidrógeno, alquilo C1-6 y haloalquilo C1-6; o R2 y R3 forman juntos un anillo cicloalquilo de C3-12; R4 está seleccionado del grupo integrado por hidrógeno, F, Cl, Br, CN, OR5, alquilo C1-4, haloalquilo C1-4 y heteroalquilo C1-4; R5 y R6 están seleccionados cada uno, de modo independiente, del grupo integrado por hidrógeno, alquilo C1-4, heteroalquilo C1-4 y haloalquilo C1-4; R7 a R9 están seleccionados cada uno, de modo independiente, del grupo integrado por hidrógeno, F, Cl, Br, I, NO2, CN, OR5, NR5R6, SR5, COR5, CO2R5, CONR5R6, alquilo C1-8, heteroalquilo C1-8, haloalquilo C1-8, alquenilo C2-8 y alquinilo C2-8; R10 a R15 están seleccionados cada uno, de modo independiente, del grupo integrado por hidrógeno, F, Cl, Br, OR5, alquilo C1-4, haloalquilo C1-4 y heteroalquilo C1-4; o R12 y R14 forman juntos un enlace, cuando Y es CR14R15; o eR12 y R14 forman juntos un enlace, cuando Z es CR14R15;Y y Z están seleccionados cada uno, de modo independiente, del grupo integrado por O, S, NR6 y CR14R15; n es 0, 1, 2 ó 3; o una sal o prodroga del mismos de aceptación farmacéutica.
AR20030102796A 2002-10-11 2003-08-04 5-(1',1'-cicloaquil/alquenil) metiliden-1,2 -dihidro-5-h-cromeno [3,4- f] quiinolinas como compuestos moduladores selectivos de receptores de progesterona AR040783A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US41814002P 2002-10-11 2002-10-11

Publications (1)

Publication Number Publication Date
AR040783A1 true AR040783A1 (es) 2005-04-20

Family

ID=32094152

Family Applications (1)

Application Number Title Priority Date Filing Date
AR20030102796A AR040783A1 (es) 2002-10-11 2003-08-04 5-(1',1'-cicloaquil/alquenil) metiliden-1,2 -dihidro-5-h-cromeno [3,4- f] quiinolinas como compuestos moduladores selectivos de receptores de progesterona

Country Status (8)

Country Link
US (2) US7084151B2 (es)
EP (1) EP1558618A1 (es)
JP (1) JP2006504736A (es)
AR (1) AR040783A1 (es)
AU (1) AU2003258047A1 (es)
CA (1) CA2501833A1 (es)
MX (1) MXPA05003800A (es)
WO (1) WO2004033459A1 (es)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6566372B1 (en) 1999-08-27 2003-05-20 Ligand Pharmaceuticals Incorporated Bicyclic androgen and progesterone receptor modulator compounds and methods
US7026484B2 (en) * 2001-02-23 2006-04-11 Ligand Pharmaceuticals Incorporated Tricyclic androgen receptor modulator compounds and methods
CL2003001544A1 (es) * 2002-10-11 2005-01-07 Ligand Pharm Inc Compuestos derivados de 5-cicloalquenil-5h-cromeno[3,4-f]quinolina de formula i, moduladores selectivos del receptor de progesterona; composicion farmaceutica; y su uso en el tratamiento de sangrado uterino disfuncional, dismenorrea, endometriosis, l
DE20301728U1 (de) 2002-10-11 2004-03-11 Ligand Pharmaceuticals, Inc., San Diego 5-substituierte 7,9-Difluor-5H-Chromeno(3,4-f) -Chinolin-Verbindungen als selektive Progesteronrezeptormodulator-Verbindungen
AR040783A1 (es) * 2002-10-11 2005-04-20 Ligand Pharm Inc 5-(1',1'-cicloaquil/alquenil) metiliden-1,2 -dihidro-5-h-cromeno [3,4- f] quiinolinas como compuestos moduladores selectivos de receptores de progesterona
CA2536349A1 (en) * 2003-08-22 2005-03-03 Ligand Pharmaceuticals Incorporated 6-cycloamino-2-quinolinone derivatives as androgen receptor modulator compounds
EP2422796A3 (en) 2006-03-07 2013-03-13 Geeta Shroff Compositions comprising human embryonic stem cells and their derivatives, methods of use, and methods of preparation
AU2008341138A1 (en) * 2007-12-20 2009-07-02 Teva Women's Health, Inc. Dosage regimens and pharmaceutical compositions and packages for emergency contraception

Family Cites Families (42)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5808139A (en) * 1992-04-21 1998-09-15 Ligand Pharmaceuticals Incorporated Non-steroid progesterone receptor agonist and antagonist and compounds and methods
US5506102A (en) * 1993-10-28 1996-04-09 Ligand Pharmaceuticals Incorporated Methods of using the A form of the progesterone receptor to screen for antagonists of steroid intracellar receptor-mediated transcription
EP1382597A3 (en) * 1994-12-22 2004-04-07 Ligand Pharmaceuticals, Inc. Steroid receptor modulator compounds and methods
US6696459B1 (en) 1994-12-22 2004-02-24 Ligand Pharmaceuticals Inc. Steroid receptor modulator compounds and methods
US5696133A (en) * 1994-12-22 1997-12-09 Ligand Pharmaceuticals Incorporated Steroid receptor modulator compounds and methods
JPH11209735A (ja) * 1998-01-28 1999-08-03 Dow Corning Toray Silicone Co Ltd フイルム状シリコーンゴム接着剤及び接着方法
US6506766B1 (en) 1998-02-13 2003-01-14 Abbott Laboratories Glucocortiocoid-selective antinflammatory agents
HUP0100460A3 (en) * 1998-02-13 2003-03-28 Ligand Pharmaceuticals Inc San Glucocorticoid-selective anti-inflammatory agents
US6380207B2 (en) * 1998-02-13 2002-04-30 Abbott Laboratories Glucocortiocoid-selective antiinflammatory agents
US6001846A (en) * 1998-02-17 1999-12-14 Ligand Pharmaceuticals Incorporated Process for the preparation of 1,2-dihydroquinolines
US6093825A (en) * 1998-05-27 2000-07-25 American Home Products Methods for preparation of 1,2-dihydroquinolines
US6093826A (en) * 1998-06-08 2000-07-25 Ligand Pharmaceuticals Incorporated Process for the preparation of C(5)-substituted 1,2-dihydro-5H-chromeno[3,4-f] quinolines
US6423699B1 (en) 1999-05-04 2002-07-23 American Home Products Corporation Combination therapies using benzimidazolones
US6498154B1 (en) 1999-05-04 2002-12-24 Wyeth Cyclic regimens using quinazolinone and benzoxazine derivatives
DE60013798T2 (de) 1999-05-04 2005-09-29 Wyeth Empfängnisverhütende zusammensetzungen die progestagen und progesteronantagonisten enthalten
US6399593B1 (en) 1999-05-04 2002-06-04 Wyeth Cyclic regimens using cyclic urea and cyclic amide derivatives
US6380178B1 (en) 1999-05-04 2002-04-30 American Home Products Corporation Cyclic regimens using cyclocarbamate and cyclic amide derivatives
US6444668B1 (en) * 1999-05-04 2002-09-03 Wyeth Combination regimens using progesterone receptor modulators
US6319912B1 (en) 1999-05-04 2001-11-20 American Home Products Corporation Cyclic regimens using 2,1-benzisothiazoline 2,2-dioxides
US6355648B1 (en) * 1999-05-04 2002-03-12 American Home Products Corporation Thio-oxindole derivatives
US6462032B1 (en) 1999-05-04 2002-10-08 Wyeth Cyclic regimens utilizing indoline derivatives
US6407101B1 (en) 1999-05-04 2002-06-18 American Home Products Corporation Cyanopyrroles
US6391907B1 (en) * 1999-05-04 2002-05-21 American Home Products Corporation Indoline derivatives
US6339098B1 (en) 1999-05-04 2002-01-15 American Home Products Corporation 2,1-benzisothiazoline 2,2-dioxides
WO2000066592A1 (en) 1999-05-04 2000-11-09 American Home Products Corporation Cyclic urea and cyclic amide derivatives
US6369056B1 (en) * 1999-05-04 2002-04-09 American Home Products Corporation Cyclic urea and cyclic amide derivatives
US6380235B1 (en) 1999-05-04 2002-04-30 American Home Products Corporation Benzimidazolones and analogues
WO2000066560A1 (en) 1999-05-04 2000-11-09 American Home Products Corporation Quinazolinone and benzoxazine derivatives as progesterone receptor modulators
US6358948B1 (en) 1999-05-04 2002-03-19 American Home Products Corporation Quinazolinone and benzoxazine derivatives as progesterone receptor modulators
US6358947B1 (en) * 1999-05-04 2002-03-19 American Home Products Corporation Tetracyclic progesterone receptor modulator compounds and methods
CN1353717A (zh) 1999-05-04 2002-06-12 莱加制药公司 四环黄体酮受体调节剂化合物及其方法
US6329416B1 (en) 1999-05-04 2001-12-11 American Home Products Corporation Combination regimens using 3,3-substituted indoline derivatives
US6306851B1 (en) 1999-05-04 2001-10-23 American Home Products Corporation Cyclocarbamate and cyclic amide derivatives
US6417214B1 (en) 1999-05-04 2002-07-09 Wyeth 3,3-substituted indoline derivatives
WO2000066168A1 (en) 1999-05-04 2000-11-09 American Home Products Corporation Compositions containing benzimidazolones and progestogens
US6509334B1 (en) 1999-05-04 2003-01-21 American Home Products Corporation Cyclocarbamate derivatives as progesterone receptor modulators
US6566372B1 (en) 1999-08-27 2003-05-20 Ligand Pharmaceuticals Incorporated Bicyclic androgen and progesterone receptor modulator compounds and methods
US6172241B1 (en) * 1999-10-15 2001-01-09 Ligand Pharmaceuticals Incorporated Process for the preparation of 1,2-dihydroquinolines
UA73119C2 (en) 2000-04-19 2005-06-15 American Home Products Corpoir Derivatives of cyclic thiocarbamates, pharmaceutical composition including noted derivatives of cyclic thiocarbamates and active ingredients of medicines as modulators of progesterone receptors
AR040783A1 (es) 2002-10-11 2005-04-20 Ligand Pharm Inc 5-(1',1'-cicloaquil/alquenil) metiliden-1,2 -dihidro-5-h-cromeno [3,4- f] quiinolinas como compuestos moduladores selectivos de receptores de progesterona
DE20301728U1 (de) 2002-10-11 2004-03-11 Ligand Pharmaceuticals, Inc., San Diego 5-substituierte 7,9-Difluor-5H-Chromeno(3,4-f) -Chinolin-Verbindungen als selektive Progesteronrezeptormodulator-Verbindungen
CL2003001544A1 (es) 2002-10-11 2005-01-07 Ligand Pharm Inc Compuestos derivados de 5-cicloalquenil-5h-cromeno[3,4-f]quinolina de formula i, moduladores selectivos del receptor de progesterona; composicion farmaceutica; y su uso en el tratamiento de sangrado uterino disfuncional, dismenorrea, endometriosis, l

Also Published As

Publication number Publication date
MXPA05003800A (es) 2005-06-08
US20040147530A1 (en) 2004-07-29
EP1558618A1 (en) 2005-08-03
AU2003258047A1 (en) 2004-05-04
US7084151B2 (en) 2006-08-01
CA2501833A1 (en) 2004-04-22
WO2004033459A1 (en) 2004-04-22
US20060223839A1 (en) 2006-10-05
JP2006504736A (ja) 2006-02-09

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