AR064477A1 - Moduladores no esteroidales del receptor de progesterona - Google Patents

Moduladores no esteroidales del receptor de progesterona

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Publication number
AR064477A1
AR064477A1 ARP070105760A ARP070105760A AR064477A1 AR 064477 A1 AR064477 A1 AR 064477A1 AR P070105760 A ARP070105760 A AR P070105760A AR P070105760 A ARP070105760 A AR P070105760A AR 064477 A1 AR064477 A1 AR 064477A1
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AR
Argentina
Prior art keywords
alkyl
ring
aryl
cycloalkyl
hydrogen
Prior art date
Application number
ARP070105760A
Other languages
English (en)
Inventor
Carsten Moeller
Ulrike Fuhrmann
Wolfgang Schwede
Anja Schmidt
Andrea Rotgeri
Thomas Andrew Kirkland
Ralf Wyrwa
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Bayer Schering Pharma Ag
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Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=39364037&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR064477(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority claimed from DE102007049630A external-priority patent/DE102007049630A1/de
Application filed by Bayer Schering Pharma Ag filed Critical Bayer Schering Pharma Ag
Publication of AR064477A1 publication Critical patent/AR064477A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D265/00Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/021,2-Oxazines; Hydrogenated 1,2-oxazines
    • 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
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/12Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
    • 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
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • 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
    • A61P5/36Antigestagens
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/02Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/32Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton containing six-membered aromatic rings
    • C07C235/38Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton containing six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00Carboxylic acid nitriles
    • C07C255/49Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C255/58Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton
    • C07C255/60Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton at least one of the singly-bound nitrogen atoms being acylated
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00Sulfones; Sulfoxides
    • C07C317/44Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton
    • C07C317/46Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton the carbon skeleton being further substituted by singly-bound oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/54Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/56Amides
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/12Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
    • C07D295/125Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/13Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/14Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D295/155Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/18Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182Radicals derived from carboxylic acids
    • C07D295/192Radicals derived from carboxylic acids from aromatic carboxylic acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D307/00Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/87Benzo [c] furans; Hydrogenated benzo [c] furans
    • C07D307/88Benzo [c] furans; Hydrogenated benzo [c] furans with one oxygen atom directly attached in position 1 or 3
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/06Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
    • C07D333/24Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/12Heterocyclic 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 chain containing hetero atoms as chain links

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

Abstract

Moduladores no esteroidales del receptor de progesterona de formula general 1, el uso de los moduladores del receptor de progesterona en la preparacion de medicamentos, y composiciones farmacéuticas que contienen estos compuestos. Los compuestos de acuerdo con la presente son apropiados para la terapia y la profilaxis de enfermedades ginecologicas, tales como la endometriosis, el leiomioma uterino, la hemorragia disfuncional y la dismenorrea, y también para la terapia y la profilaxis de tumores dependientes de hormonas, y para usarlos en el control de la fertilidad femenina y la terapia de reemplazo de hormonas femeninas. Reivindicacion 1: Compuestos de la formula general 1 caracterizados porque q es 0 o 1, R1 representa arilo C6- 12 mono o bicíclico, un heteroarilo de entre 5 y 12 miembros, cicloalquilo C3-10 o un radical heterocíclico de entre 3 y 10 miembros, que puede no estar sustituido o puede estar opcionalmente sustituido con hasta 3 radicales, donde cada uno de los sustituyentes tiene independientemente uno de los siguientes significados: alquilo C1-8, alquenilo C2-8, alquinilo C2-8, alquilo C1-6 parcial o completamente fluorado, alcoxilo C1-6 parcial o completamente fluorado, alcoxi C1-6-alquilo C1-6, alcoxi C1-6-alcoxilo C1-6, (CH2)p-cicloalquilo C3-10, (CH2)p-heterocicloalquilo, (CH2)pCN, (CH2)pHal, (CH2)pNO2, (CH2)p-arilo C6-12 opcionalmente sustituido con Z, (CH2)p-heteroarilo opcionalmente sustituido con Z, -(CH2)pPO3(Rb)2, -(CH2)pNRcRd, - (CH2)pNReCORb, -(CH2)pNReCSRb, -(CH2)pNReS(O)Rb, -(CH2)pNReS(O)2Rb, -(CH2)pNReCONRcRd, -(CH2)pNReCOORb, -(CH2)pNReC(NH)nRcRd, -(CH2)pNReCSNRcRd, -(CH2)pNReS(O)RcRd, -(CH2)pNReS(O)2NRcRd, -(CH2)pCORb, -(CH2)pCSRb, -(CH2)pS(O)Rb, -(CH2)pS(O)(NH)Rb, - (CH2)pS(O)2Rb, -(CH2)pS(O)2NRcRd, - (CH2)pSO2ORb, -(CH2)pCO2Rb, -(CH2)pCONRcRd, -(CH2)pCSNRcRd, -(CH2)pORb, (CH2)pSRb, -(CH2)pCRb(OH)-Rb, -(CH2)pC=NORb, -O-(CH2)n-O-, -O-(CH2)n-CH2-, -O-CH=CH- o -(CH2)n+2-, donde n es 1 o 2, y el resto de los átomos de oxígeno y/o carbono están unidos con los átomos de carbono del anillo directamente adyacentes, y p es 0, 1, 2, 3, 4, 5 o 6, y Z representa ciano, halogeno, nitro, -(CH2)pORb, - (CH2)pS(O)2Rb, -C(O)Rb, CO2Rb, -O-Rb, -S-Rb, SO2NRcRd, - C(O)NRcRd, -OC(O)-NRcRd, -C=NORb, -NRcRd, alquilo C1-6 parcial o completamente fluorado, o alcoxilo C1-6 parcial o completamente fluorado, Rb representa hidrogeno o alquilo C1-6, alquenilo C2-8, alquinilo C2-8, cicloalquilo C3-10, arilo C6-12 o alquilo C1- 3 parcial o completamente fluorado, Rc y Rd representan independientemente hidrogeno, alquilo C1-6 opcionalmente sustituido con W, alquenilo C2-8, alquinilo C2-8, cicloalquilo C3-10, arilo C6-12, un radical heteroarilo de entre 5 y 12 miembros, C(O)Rb o un grupo hidroxilo, y W representa -NRfRg, donde Rf representa hidrogeno o alquilo C1-3 y Rg representa hidrogeno o alquilo C1-3, o Rf y Rg, junto con el nitrogeno, forman un anillo de entre 3 y 7 miembros, que opcionalmente está ampliado con O, S o NRh, donde Rh representa hidrogeno, alquilo C1-3, alcanoilo C1-3, alquilsulfonilo C1-3, o alcoxicarbonilo C1-3, donde cuando Rc es un grupo hidroxilo, Rd solamente puede ser hidrogeno, alquilo C1-6, alquenilo C2-8, alquinilo C2- 8, cicloalquilo C3-10 o arilo C6-12, y viceversa, y también Re representa hidrogeno, alquilo C1-6, alquenilo C2-8, alquinilo C2-8, cicloalquilo C3-10 o arilo C6-12, R2 representa arilo C6-12 mono o bicíclico, o un radical heteroarilo de entre 5 y 12 miembros, que no está sustituido u opcionalmente puede estar sustituido con hasta 3 de los radicales mencionados para R1, R3 tiene los significados indicados para R2, o representa uno de los siguientes grupos A o B: A: Sistemas de anillo-6/anillo-6 union con las estructuras basales en la posicion 5, 6, 7 u 8, B: Sistemas de anillo-6/anillo-5: union con las estructuras basales en la posicion 4, 5, 6 o 7 donde R4 representa hidrogeno o alquilo C1-4, o alquilo C1-4 parcial o completamente fluorado, R5a y R5b representan independientemente hidrogeno, alquilo C1-4 o alquilo C1-4 parcial o completamente fluorado, o junto con el átomo de carbono del anillo, forman un anillo de entre 3 y 6 miembros, y también X representa oxígeno o dos átomos de hidrogeno, Y representa -(CH2)m-, -C:::C- o -CH=CH-, y m es 0 o 1, y sus sales aceptables para el uso farmacéutico.
ARP070105760A 2006-12-21 2007-12-20 Moduladores no esteroidales del receptor de progesterona AR064477A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE102006061912 2006-12-21
DE102007049630A DE102007049630A1 (de) 2007-10-11 2007-10-11 Nichtsteroidale Progesteronrezeptor-Modulatoren

Publications (1)

Publication Number Publication Date
AR064477A1 true AR064477A1 (es) 2009-04-01

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ID=39364037

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ARP070105760A AR064477A1 (es) 2006-12-21 2007-12-20 Moduladores no esteroidales del receptor de progesterona

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AR (1) AR064477A1 (es)
CL (1) CL2007003769A1 (es)
TW (1) TW200835499A (es)
UY (1) UY30815A1 (es)
WO (1) WO2008077646A1 (es)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111825605B (zh) * 2019-04-19 2023-03-31 中国科学院上海药物研究所 芳基酮酰胺类化合物及其制备方法和用途

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE19723722A1 (de) * 1997-05-30 1998-12-10 Schering Ag Nichtsteroidale Gestagene
EP1344776A1 (en) * 2002-03-11 2003-09-17 Schering Aktiengesellschaft 5- 2-hydroxy-3-[1-(3-trifluoromethylphenyl)-cyclopropyl]-propionylamino -phtalide and 6- 2-hydroxy-3-[1-(3-trifluoromethylphenyl)-cyclopropyl]-propionylamino -4-methyl-2,3-benzoxazin-1-one derivatives with progesterone receptor modulating activity for use in fertility control, hormone replacement therapy and the treatment of gynecological disorders

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CL2007003769A1 (es) 2008-08-08
WO2008077646A1 (de) 2008-07-03
TW200835499A (en) 2008-09-01
UY30815A1 (es) 2008-07-31

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