AR064477A1 - NON-STEROID MODULATORS OF THE PROGESTERONE RECEIVER - Google Patents

NON-STEROID MODULATORS OF THE PROGESTERONE RECEIVER

Info

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
Authority
AR
Argentina
Prior art keywords
alkyl
ring
aryl
cycloalkyl
hydrogen
Prior art date
Application number
ARP070105760A
Other languages
Spanish (es)
Inventor
Carsten Moeller
Ulrike Fuhrmann
Wolfgang Schwede
Anja Schmidt
Andrea Rotgeri
Thomas Andrew Kirkland
Ralf Wyrwa
Original Assignee
Bayer Schering Pharma Ag
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
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/en
Application filed by Bayer Schering Pharma Ag filed Critical Bayer Schering Pharma Ag
Publication of AR064477A1 publication Critical patent/AR064477A1/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/02—1,2-Oxazines; Hydrogenated 1,2-oxazines
    • 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
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • 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
    • A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • 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
    • A61P5/36—Antigestagens
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/02—Carboxylic 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
    • C07C235/32—Carboxylic 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
    • C07C235/38—Carboxylic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00—Carboxylic acid nitriles
    • C07C255/49—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C255/58—Carboxylic 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
    • C07C255/60—Carboxylic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00—Sulfones; Sulfoxides
    • C07C317/44—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton
    • C07C317/46—Sulfones; 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic 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
    • C07D213/02—Heterocyclic 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
    • C07D213/04—Heterocyclic 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
    • C07D213/24—Heterocyclic 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
    • C07D213/54—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/56—Amides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic 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
    • C07D295/04—Heterocyclic 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
    • C07D295/12—Heterocyclic 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
    • C07D295/125—Heterocyclic 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
    • C07D295/13—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic 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
    • C07D295/04—Heterocyclic 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
    • C07D295/14—Heterocyclic 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
    • C07D295/155—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic 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
    • C07D295/16—Heterocyclic 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
    • C07D295/18—Heterocyclic 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
    • C07D295/182—Radicals derived from carboxylic acids
    • C07D295/192—Radicals derived from carboxylic acids from aromatic carboxylic acids
    • 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
    • C07D307/77—Heterocyclic 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
    • C07D307/87—Benzo [c] furans; Hydrogenated benzo [c] furans
    • C07D307/88—Benzo [c] furans; Hydrogenated benzo [c] furans with one oxygen atom directly attached in position 1 or 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic 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
    • C07D333/06—Heterocyclic 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
    • C07D333/24—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • 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
    • C07D413/12—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 chain containing hetero atoms as chain links

Landscapes

  • 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.Non-steroidal progesterone receptor modulators of general formula 1, the use of progesterone receptor modulators in the preparation of medicaments, and pharmaceutical compositions containing these compounds. The compounds according to the present are suitable for the therapy and prophylaxis of gynecological diseases, such as endometriosis, uterine leiomyoma, dysfunctional hemorrhage and dysmenorrhea, and also for the therapy and prophylaxis of hormone-dependent tumors, and for use in female fertility control and female hormone replacement therapy. Claim 1: Compounds of the general formula 1 characterized in that q is 0 or 1, R1 represents mono or bicyclic C6-12 aryl, a 5-12 membered heteroaryl, C3-10 cycloalkyl or a 3-10 membered heterocyclic radical , which may not be substituted or may be optionally substituted with up to 3 radicals, where each of the substituents independently has one of the following meanings: C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, partial C1-6 alkyl or completely fluorinated, C1-6 alkoxy partially or completely fluorinated, C1-6 alkoxy-C1-6 alkyl, C1-6 alkoxy-C1-6 alkoxy, (CH2) p-C3-10 cycloalkyl, (CH2) p-heterocycloalkyl, (CH2) pCN, (CH2) pHal, (CH2) pNO2, (CH2) C6-12 p-aryl optionally substituted with Z, (CH2) p-heteroaryl optionally substituted with 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, - (CH 2) 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) nO-, -O- (CH2) n-CH2-, -O- CH = CH- or - (CH2) n + 2-, where n is 1 or 2, and the rest of the oxygen and / or carbon atoms are attached to the directly adjacent ring carbon atoms, and p is 0.1 , 2, 3, 4, 5 or 6, and Z represents cyano, halogen, 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, partial or fully fluorinated C1-6 alkyl, or partially or completely fluorinated C1-6 alkoxy, Rb represents hydrogen or C1-6 alkyl, C2-8 alkenyl, C2-8 alkynyl, C3-10 cycloalkyl, C6-12 aryl or partially or fully fluorinated C1-3 alkyl, Rc and Rd independently represent hydrogen, optionally substituted C1-6 alkyl with W, C2-8 alkenyl, alkyl C2-8 nyl, C3-10 cycloalkyl, C6-12 aryl, a 5- to 12-membered heteroaryl radical, C (O) Rb or a hydroxyl group, and W represents -NRfRg, where Rf represents hydrogen or C1-3 alkyl and Rg represents hydrogen or C1-3 alkyl, or Rf and Rg, together with the nitrogen, form a ring of between 3 and 7 members, which is optionally extended with O, S or NRh, where Rh represents hydrogen, C1-3 alkyl , C1-3 alkanoyl, C1-3 alkylsulfonyl, or C1-3 alkoxycarbonyl, where when Rc is a hydroxyl group, Rd can only be hydrogen, C1-6 alkyl, C2-8 alkenyl, C2-8 alkynyl, C3-10 cycloalkyl or C6-12 aryl, and vice versa, and also Re represents hydrogen, C1-6 alkyl, C2-8 alkenyl, C2-8 alkynyl, C3-10 cycloalkyl or C6-12 aryl, R2 represents mono or bicyclic C6-12 aryl, or a 5- to 12-membered heteroaryl radical, which is not substituted or can optionally be substituted with up to 3 of the radicals mentioned for R1, R3 has the meanings indicated for R2 , or represents one of the following groups A or B: A: Ring-6 / ring-6 union systems with the basal structures in position 5, 6, 7 or 8, B: Ring-6 / ring-5 systems : union with the basal structures at position 4, 5, 6 or 7 where R4 represents hydrogen or C1-4 alkyl, or partially or completely fluorinated C1-4 alkyl, R5a and R5b independently represent hydrogen, C1-4 alkyl or C1 alkyl -4 partially or completely fluorinated, or together with the carbon atom of the ring, form a ring of 3 to 6 members, and also X represents oxygen or two hydrogen atoms, Y represents - (CH2) m-, -C: :: C- or -CH = CH-, and m is 0 or 1, and its salts acceptable for pharmaceutical use.

ARP070105760A 2006-12-21 2007-12-20 NON-STEROID MODULATORS OF THE PROGESTERONE RECEIVER AR064477A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE102006061912 2006-12-21
DE102007049630A DE102007049630A1 (en) 2007-10-11 2007-10-11 New amide compounds used for therapy and/or prophylaxis of gynecological diseases e.g. endometriosis, for female fertility control and female hormone replacement therapy

Publications (1)

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

Family

ID=39364037

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP070105760A AR064477A1 (en) 2006-12-21 2007-12-20 NON-STEROID MODULATORS OF THE PROGESTERONE RECEIVER

Country Status (5)

Country Link
AR (1) AR064477A1 (en)
CL (1) CL2007003769A1 (en)
TW (1) TW200835499A (en)
UY (1) UY30815A1 (en)
WO (1) WO2008077646A1 (en)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111825605B (en) * 2019-04-19 2023-03-31 中国科学院上海药物研究所 Aryl ketone amide compound and preparation method and application thereof

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE19723722A1 (en) * 1997-05-30 1998-12-10 Schering Ag Nonsteroidal progestogens
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

Also Published As

Publication number Publication date
WO2008077646A1 (en) 2008-07-03
UY30815A1 (en) 2008-07-31
TW200835499A (en) 2008-09-01
CL2007003769A1 (en) 2008-08-08

Similar Documents

Publication Publication Date Title
ES2703552T3 (en) New pyrimidine derivatives fused for the inhibition of tyrosine kinase activity
AR047890A1 (en) DERIVATIVES OF AZABICICLO [3.1.0] HEXANO AS MODULATORS OF DOPAMINE D3 RECEIVERS
PE20171240A1 (en) DERIVATIVES OF 4H-PYRROL [3,2-C] PYRIDIN-4-ONA
AR030306A1 (en) PIPERAZINE DERIVATIVES, A PROCEDURE FOR THE PREPARATION, PHARMACEUTICAL COMPOSITIONS, A METHOD FOR THE MANUFACTURE AND THE USE OF SUCH DERIVATIVES FOR THE MANUFACTURE OF A MEDICINAL PRODUCT
AR091416A1 (en) DIAZAESPIROCICLOALCANOS AND AZAESPIROCICLOALCANOS AS INHIBITORS OF ATX AND LPA
AR049346A1 (en) 3-AMINO-1-ARILPROPIL-INDOLES AS MONOAMINE REABSORTION INHIBITORS
AR080785A1 (en) DERIVATIVES OF IMIDAZO [1,2-A] PYRIMIDINE, PROCESS TO PREPARE THEM AND INTERMEDIARIES OF SUCH SYNTHESIS, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND USE OF THEM IN THE TREATMENT OF PATHOLOGIES OF THE CENTRAL NERVOUS SYSTEM, SUCH AS PARK AND OTHERS.
AR071857A1 (en) DERIVATIVES OF INDAZOL REPLACED WITH PHENYL AND BENZODIOXINYL, A PHARMACEUTICAL COMPOSITION THAT INCLUDES THEM AND ITS USE IN THE MANUFACTURE OF A MEDICINAL PRODUCT FOR THE TREATMENT OF DISEASES MEDIATED BY THE GLUCOCORTICOID RECEPTOR.
AR051753A1 (en) METHODS TO PREPARE INDAZOL COMPOUNDS
AR049711A1 (en) HETEROCICLIC COMPOUNDS CONDENSED AS INHIBITORS OF ALDOSTERONE SINTASA; PHARMACEUTICAL COMPOSITIONS THAT CONTAIN THEM AND THEIR USE IN THE PREPARATION OF A MEDICINAL PRODUCT FOR THE TREATMENT OR PREVENTION OF DISEASES RELATED TO HYPERALDOSTERISM AND EXCESSIVE CORTISO RELEASE
AR088218A1 (en) USEFUL HETEROCICLICAL COMPOUNDS AS PI3K INHIBITORS
ES2714100T3 (en) Fused quinoline compounds as mTor inhibitors, pi3k
AR074583A1 (en) 4-AZETIDINIL-1-HETEROARIL-CICLOHEXANOL ANTAGONISTS OF CCR2
AR059831A1 (en) SUBSTITUTED CHROMANOL DERIVATIVES
AR065891A1 (en) DERIVATIVES OF PYRIDINE AND PYRIMIDINE AS ANTAGONISTS OF MGLUR2
AR046603A1 (en) DIHYDROBENZOFURANILO ALKANAMINS AND METHODS FOR USE AS PHARMACES IN THE CNS
AR051325A1 (en) BIARILQUINOLIN-4-ILAMINA SUBSTITUTED ANALOGS
AR048717A1 (en) DERIVATIVES OF HEXENOIC ACID, PROCEDURES FOR THEIR PREPARATION, PHARMACEUTICAL COMPOSITIONS THAT INCLUDE THEM AND THEIR THERAPEUTIC APPLICATIONS
ES2409404T3 (en) Heterocyclic phenoxymethyl compounds
PE20121743A1 (en) TRICYCLIC PYRIDINE DERIVATIVES, DRUGS CONTAINING SUCH COMPOUNDS, THEIR USE AND PROCESS FOR THEIR PREPARATION
AR069813A1 (en) DERIVATIVES OF 2- AMINO-PYRIMIDINE, A PHARMACEUTICAL COMPOSITION, A METHOD OF PREPARATION OF THE COMPOUND AND USE OF IT TO PREPARE A MEDICINAL PRODUCT
AR085920A1 (en) USEFUL BENZIMIDAZOLIC DERIVATIVES AS ANTITUMOR AGENTS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
ES2901829T3 (en) Substituted azaindoline derivatives as NIK inhibitors
AR044662A1 (en) AZETIDINE COMPOUNDS
ES2606839T3 (en) Tetraaza-cyclopenta [a] indenyl and its use as positive allosteric modulators

Legal Events

Date Code Title Description
FB Suspension of granting procedure