AR078538A1 - Pirroles e imidazoles sustituidos como ligandos del receptor de estrogenos - Google Patents

Pirroles e imidazoles sustituidos como ligandos del receptor de estrogenos

Info

Publication number
AR078538A1
AR078538A1 ARP100103631A ARP100103631A AR078538A1 AR 078538 A1 AR078538 A1 AR 078538A1 AR P100103631 A ARP100103631 A AR P100103631A AR P100103631 A ARP100103631 A AR P100103631A AR 078538 A1 AR078538 A1 AR 078538A1
Authority
AR
Argentina
Prior art keywords
6alkyl
group
phenyl
6alkenyl
benzyl
Prior art date
Application number
ARP100103631A
Other languages
English (en)
Original Assignee
Karobio Ab
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
Priority claimed from GB0917576A external-priority patent/GB0917576D0/en
Priority claimed from GBGB1011859.4A external-priority patent/GB201011859D0/en
Application filed by Karobio Ab filed Critical Karobio Ab
Publication of AR078538A1 publication Critical patent/AR078538A1/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
    • C07D231/12—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 only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • 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
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • 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
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/20—Hypnotics; Sedatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two 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
    • C07D207/36—Oxygen or sulfur atoms
    • C07D207/40—2,5-Pyrrolidine-diones
    • C07D207/416—2,5-Pyrrolidine-diones 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 other ring carbon atoms
    • 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
    • C07D231/38—Nitrogen atoms
    • 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
    • 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
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • 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
    • C07D413/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Immunology (AREA)
  • Reproductive Health (AREA)
  • Endocrinology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Gynecology & Obstetrics (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Urology & Nephrology (AREA)
  • Diabetes (AREA)
  • Hospice & Palliative Care (AREA)
  • Ophthalmology & Optometry (AREA)
  • Child & Adolescent Psychology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Anesthesiology (AREA)
  • Transplantation (AREA)
  • Vascular Medicine (AREA)

Abstract

Un éster, amida, solvato o su sal farmacéuticamente aceptable, Incluyendo una sal de tal éster o amida, y un solvato de tal éster, amida o sal. También proporciona el uso de tales compuestos en el tratamiento o profilaxis de una afeccion asociada con una enfermedad o trastorno asociado con la actividad del receptor de estrogenos. Reivindicacion 1: Un compuesto de formula (1) o un éster, amida, solvato o su sal farmacéuticamente aceptable, incluyendo una sal de tal éster o amida, y un solvato de tal éster, amida o sal, donde G representa el grupo: (2) donde tanto uno de A, B, D y E representa nitrogeno, o los dos de A y D representan nitrogeno, y los otros de A, B, D y E representan carbono; R1 se selecciona del grupo integrado por halogeno, ciano, nitro, ORA, N(RB)2, -C(O)C1-4alquilo, -SO2C1-4alquilo, C1-8alquilo, C2-8alquenilo, C2-8alquinilo, haloC1-8alquilo, dihaIoC1-8alquiIo, trihaloC1-8alquilo, haloC2-8alquenilo, dihaloC2-8alquenilo, trihaloC2-8alquenilo, cianoC1-8alquilo, C1-4alcoxiC1-8 alquilo, C3-8cicloalquilo, C3-8cicloalquilC1-8alquilo, fenilo, bencilo, y heterociclilo de 5 a 10 miembros, donde dicho grupo bencilo o heterociclilo es ya sea no sustituido o dicho grupo fenilo, bencilo o heterociclilo es sustituido con desde 1 a 3 sustituyentes, cada sustituyente siendo seleccionado de manera independiente del grupo integrado por ORA, N(RB)2, halogeno, ciano, nitro, -C(O)C1-4alquilo, C1-6alquilo, C2-6alquenilo, C2-6alquinilo, haloC1-6alquilo, dihaloC1-6aIquilo y trihaloC1-6alquilo; R2 se selecciona del grupo integrado por hidrogeno, halogeno, ciano, nitro, ORA, N(RB)2, N(OH)2, -CHO, -CH=N-OH, -C(O)C1-4alquilo opcionalmente sustituido con desde 1 a 3 halogenos, -SO2C1-4alquilo, -C(O)NH-OH, -C(NH2)=N-OH, -C(CO2H)=N-OH, -C(O-C1-4alquil)=NH, -C(NH2)=N-NH2, -NH-C(NH2)=NH, -NH-C(O)NH2, -N=C(-NH-CH2CH2-NH-), -S-CN, -S-C(NH2)=NH, -S-C(NH2)=N-OH, -CO2H, -CH2-CO2H, -CH(OH)CO2H, -C(O)N(RC)2, SO2N(RC)2, -C(O)-C(O)-NH2, -CH2NH-CONH2, NHSO2RB, C1-6alquil-NH2, C1-6aIquil-OH, -C(O)CO2H, SO3H, -CH2SO3H, C1-6alquiIo, haIoC1-6alquilo, dihaloC1-6alquilo, trihaloC1-6alquiIo, cianoC1-6alquilo, C1-4alcoxiC1-6aIquilo, C2-6alquenilo, C2-6alquinilo, C3-8cicloalquilo, C3-8cicloaIquilC1-6 alquilo, fenilo, bencilo y heterociclilo de 5 a 10 miembros donde dicho grupo fenilo, bencilo o heterociclilo puede ser tanto no sustituido o sustituido con desde 1 a 3 sustituyentes cada sustituyente siendo seleccionado del grupo integrado por ORA, halogeno, ciano, nitro, C1-6alquilo, C2-6alquenilo, C2-6alquinilo, haloC1-6alquilo, dihaloC1-6alquilo y trihaloC1-6alquilo; cada uno de R3B y R3D es de manera independiente seleccionado del grupo integrado por hidrogeno, halogeno, C1-6alquilo, C2-6alquenilo, C2-6alquinilo, C3-8cicloalquilo, C3-8cicIoalquiIC1-6alquilo; haloC1-6alquilo, dihaloC1-6aIquilo, trihaloC1-6alquilo, fenilo, bencilo y heterociclilo de 5 a 10 miembros donde dicho grupo bencilo o heterociclilo es ya sea no sustituido o dicho grupo fenilo, bencilo o heterociclilo es sustituido con desde 1 a 3 sustituyentes cada sustituyente siendo de manera independiente seleccionado del grupo integrado por ORA, halogeno, ciano, nitro, C1-6alquilo, C2-6alquenilo, C2-6aIquinilo, haloC1-6alquilo, dihaloC1-6alquilo y trihaloC1-6alquilo; o R3B o R3D está ausente cuando se liga a un nitrogeno que forma un doble enlace con un átomo de carbono adyacente; y donde solamente uno de R1, R2, R3B y R3D puede ser simultáneamente un fenilo sustituido o no sustituido; cada uno de R4, R5, R6 y R7 es de manera independiente seleccionado del grupo integrado por hidrogeno, ORA, halogeno, ciano, nitro, C1-6alquilo, C2-6alquenilo, C2-6alquinilo, haloC1-6alquilo, dihaIoC1-6aIquilo y trihaloC1-6alquilo; cada RA es de manera independiente seleccionado del grupo integrado por hidrogeno, C1-6alquilo, C2-6alquenilo, C2-6aIquiniIo, C3-8cicloaIquilo, C3-8cicloalquilC1-6alquilo, fenilo, bencilo y heterociclilo de 5 a 10 miembros, cada uno opcionalmente sustituido por desde 1 a 3 átomos de halogeno; cada RB es de manera independiente seleccionado del grupo integrado por hidrogeno, C1-6alquilo, C2-6alquenilo, C2-6alquinilo, C3-8cicloalquilo, C3-8cicloalquilC1-6alquilo, fenilo, bencilo y heterociclilo de 5 a 10 miembros, cada uno opcionalmente sustituido por desde 1 a 3 átomos de halogeno; y cada RC es de manera independiente seleccionado del grupo integrado por hidrogeno y C1-6alquilo; siempre que el compuesto de formula 1 no sea 3-cloro-4-(4-nitro-1H-pirrol-3-il)fenol.
ARP100103631A 2009-10-07 2010-10-06 Pirroles e imidazoles sustituidos como ligandos del receptor de estrogenos AR078538A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB0917576A GB0917576D0 (en) 2009-10-07 2009-10-07 Novel estrogenreceptor ligands
GBGB1011859.4A GB201011859D0 (en) 2010-07-14 2010-07-14 Novel estrogen receptor ligands

Publications (1)

Publication Number Publication Date
AR078538A1 true AR078538A1 (es) 2011-11-16

Family

ID=43856389

Family Applications (2)

Application Number Title Priority Date Filing Date
ARP100103629A AR078536A1 (es) 2009-10-07 2010-10-06 Derivados de pirazol como ligandos del receptor de estrogeno
ARP100103631A AR078538A1 (es) 2009-10-07 2010-10-06 Pirroles e imidazoles sustituidos como ligandos del receptor de estrogenos

Family Applications Before (1)

Application Number Title Priority Date Filing Date
ARP100103629A AR078536A1 (es) 2009-10-07 2010-10-06 Derivados de pirazol como ligandos del receptor de estrogeno

Country Status (10)

Country Link
US (2) US8653112B2 (es)
EP (1) EP2486018B1 (es)
JP (1) JP5735518B2 (es)
CN (1) CN102648183B (es)
AR (2) AR078536A1 (es)
DK (1) DK2486018T3 (es)
ES (1) ES2737429T3 (es)
IN (1) IN2012DN02556A (es)
TW (2) TW201124409A (es)
WO (2) WO2011042475A1 (es)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB201113538D0 (en) 2011-08-04 2011-09-21 Karobio Ab Novel estrogen receptor ligands
WO2013079223A1 (en) 2011-12-02 2013-06-06 Phenex Pharmaceuticals Ag Pyrrolo carboxamides as modulators of orphan nuclear receptor rar-related orphan receptor-gamma (rorϒ, nr1f3) activity and for the treatment of chronic inflammatory and autoimmune diseases
CN102558058B (zh) * 2012-01-19 2014-10-29 陕西理工学院 1-芳基-3-取代-5-取代氨基-4-吡唑甲酰胺类化合物及其应用
JO3215B1 (ar) 2012-08-09 2018-03-08 Phenex Pharmaceuticals Ag حلقات غير متجانسة بها 5 ذرات تحتوي على النيتروجين بها استبدال بكربوكساميد أو سلفوناميد كمعدلات لمستقبل نووي غير محمي RORy
US9944597B2 (en) 2013-09-16 2018-04-17 The Board Of Regents Of The University Of Texas System Polysubstituted pyrroles having microtubule-disrupting, cytotoxic and antitumor activities and methods of use thereof
WO2015070366A1 (en) 2013-11-12 2015-05-21 Merck Sharp & Dohme Corp. Aryl linked imidazole and triazole derivatives and methods of use thereof for improving the pharmacokinetics of a drug
US9974776B2 (en) 2013-12-05 2018-05-22 Karo Pharma Ab Estrogen receptor beta agonists for use in treating mesothelioma
CN104974091B (zh) * 2014-04-10 2018-01-02 沈阳药科大学 3‑甲基‑1,5‑二芳基吡唑类化合物及其制备方法和用途
US10758496B2 (en) 2014-09-02 2020-09-01 The Regents Of The University Of California Estrogen receptor ligand treatment for neurodegenerative diseases
WO2016097036A1 (en) * 2014-12-17 2016-06-23 Karo Bio Ab Estrogen receptor ligand for use in treating melanoma
CN106397377B (zh) * 2016-09-05 2019-04-05 中南大学 一种富电子五元杂环酸及其衍生物脱羧上氟的方法
WO2018205928A1 (zh) 2017-05-09 2018-11-15 杭州安道药业有限公司 吲哚嗪衍生物及其在医药上的应用
CN108610246A (zh) * 2018-06-01 2018-10-02 山东潍坊润丰化工股份有限公司 一种环丙唑醇中间体1-（4-氯苯基）-2-环丙基-1-丙酮的制备方法
WO2021057998A1 (zh) * 2019-09-29 2021-04-01 上海森辉医药有限公司 一种吡咯并氨基哒嗪酮化合物的制备方法

Family Cites Families (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5726653A (en) * 1980-05-09 1982-02-12 Ciba Geigy Ag Substituted phenyl ether
JPS58208275A (ja) * 1982-05-20 1983-12-03 Lion Corp ５−アミノ−ピラゾ−ル誘導体及び該化合物を含有する抗腫瘍剤
US5096919A (en) * 1989-01-05 1992-03-17 Ciba-Geigy Corporation Pyrrolylphenyl-substituted hydroxamic acid derivatives
CA2219269A1 (en) 1996-10-29 1998-04-29 Novartis Ag Novel herbicides
DE69935335T2 (de) 1998-08-07 2007-11-22 Novartis Vaccines and Diagnostics, Inc., Emeryville Pyrazole als modulatoren des östrogenrezeptors
AU1199600A (en) * 1998-10-02 2000-04-26 Board Of Trustees Of The University Of Illinois, The Estrogen receptor ligands
AU2001258784A1 (en) * 2000-05-22 2001-12-03 Takeda Chemical Industries Ltd. Tyrosine phosphatase inhibitors
DE60222804T2 (de) * 2001-12-21 2008-07-03 Vernalis (Cambridge) Ltd., Abington 3-(2,4)dihydroxyphenyl-4-phenylpyrazole und deren medizinische verwendung
US6835745B2 (en) * 2002-01-15 2004-12-28 Wyeth Phenyl substituted thiophenes as estrogenic agents
GB0229618D0 (en) * 2002-12-19 2003-01-22 Cancer Rec Tech Ltd Pyrazole compounds
EP1633699B1 (en) * 2003-05-16 2007-01-03 Wyeth Aryl-carbaldehyde oxime derivatives and their use as estrogenic agents
US7250440B2 (en) * 2003-08-12 2007-07-31 Wyeth (Hydroxyphenyl)-1H-indole-3-carbaldehyde oxime derivatives as estrogenic agents
US20070191336A1 (en) 2003-12-24 2007-08-16 Flynn Daniel L Anti-inflammatory medicaments
CN101061116A (zh) 2004-09-24 2007-10-24 詹森药业有限公司 磺酰胺化合物
JP2006316054A (ja) * 2005-04-15 2006-11-24 Tanabe Seiyaku Co Ltd 高コンダクタンス型カルシウム感受性ｋチャネル開口薬
JP2006306755A (ja) 2005-04-27 2006-11-09 Nippon Kayaku Co Ltd 新規なピラゾール誘導体とそれを有効成分とするｈｓｐ９０阻害剤
EP1889617A1 (en) 2006-07-11 2008-02-20 Freie Universität Berlin Triphenyl modified 5-membered heterocycles and their use as anticancer and antiflammatory agents
EP2074102A1 (en) 2006-10-13 2009-07-01 Karo Bio Ab 2-phenyl indene derivatives useful as estrogen receptor ligands
WO2009012954A1 (en) 2007-07-20 2009-01-29 Karo Bio Ab Novel estrogen receptor ligands
CA2695812A1 (en) 2007-08-08 2009-02-12 Neurosearch A/S Novel 1,2,3-triazole derivatives useful as modulators of nicotinic acetylcholine receptors
GB0806656D0 (en) 2008-04-11 2008-05-14 Karobio Ab Novel estrogen receptor ligands
DK2276732T3 (en) 2008-04-16 2015-08-17 Karobio Ab Novel østrogenreceptorligander
GB0817221D0 (en) 2008-09-19 2008-10-29 Karobio Ab Novel estrogen receptor ligands

Also Published As

Publication number Publication date
CN102648183A (zh) 2012-08-22
IN2012DN02556A (es) 2015-08-28
TW201124406A (en) 2011-07-16
ES2737429T3 (es) 2020-01-14
JP2013507336A (ja) 2013-03-04
DK2486018T3 (da) 2019-07-29
JP5735518B2 (ja) 2015-06-17
EP2486018B1 (en) 2019-04-24
US8921402B2 (en) 2014-12-30
US8653112B2 (en) 2014-02-18
US20120202853A1 (en) 2012-08-09
WO2011042477A1 (en) 2011-04-14
TW201124409A (en) 2011-07-16
EP2486018A1 (en) 2012-08-15
CN102648183B (zh) 2015-12-02
US20140128435A1 (en) 2014-05-08
WO2011042475A1 (en) 2011-04-14
AR078536A1 (es) 2011-11-16

Similar Documents

Publication Publication Date Title
AR078538A1 (es) Pirroles e imidazoles sustituidos como ligandos del receptor de estrogenos
AR078535A1 (es) Derivados de pirrolo[2,3-b]piridina ligandos de receptores estrogenicos, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de la osteoporosis y enfermedades del sistema nervioso central, entre otras
CO6260076A2 (es) Derivados de uracilo o timina para el tratamiento de la hepatitis c
AR072952A1 (es) Compuestos de 2-imino-3-metilpirrolopirimidinona fenilo-sustituida como inhibidores de bace-1, composiciones y su uso
AR062074A1 (es) Derivados de alcoholes 1-fenil-2-piridinil alquilenicos como inhibidores de fosfodiesterasa
EA200970461A1 (ru) ЗАМЕЩЕННЫЕ ПРОИЗВОДНЫЕ 3-ИЗОБУТИЛ-9,10-ДИМЕТОКСИ-1,3,4,6,7,11b-ГЕКСАГИДРО-2Н-ПИРИДО[2,1-a]ИЗОХИНОЛИН-2-ОЛА И СВЯЗАННЫЕ С НИМИ СПОСОБЫ
RS54165B1 (en) NEW LIGANDS FOR THE ESTROGENIC RECEPTOR
AR049646A1 (es) Derivados de sulfamato y sulfamida utiles para el tratamiento de la epilepsia y trastornos relacionados
AR078151A1 (es) Conjugados de acidos grasos y niacina, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de enfermedades metabolicas.
AR069490A1 (es) Agonistas de los receptores de glucocorticoides
TR201903556T4 (tr) Muskarinik reseptör antagonisti ve beta 2 adrenerjik reseptör agonisti aktivitesine sahip diamid bileşikleri.
CL2012000999A1 (es) Compuestos derivados de pirazoloespirocetona sustituida, inhibidores de acetil-coa carboxilasa; composicion farmaceutica que los comprende; uso para tratar o retrasar la progresion o el inicio de diabetes tipo 2, higado graso no alcoholico (hgna) o la resistencia hepatica a la insulina.
AR059622A1 (es) Quinolonas utiles como inhibidores de la sintetasa del oxido nitrico inducibles
AR061815A1 (es) Compuesto de oxo-prolinamida composicion farmaceutica que lo comprende y su uso para la elaboracion de un medicamento
AR049398A1 (es) Derivados de sulfamato y sulfamida; una composicion farmaceutica que los contiene y su uso en la preparacion de un medicamento util para el tratamiento de la epilepsia y trastornos relacionados.
AR038686A1 (es) Formulaciones de derivados de androstano y agonistas del adrenoreceptor beta 2 antiinflamatorios
AR065280A1 (es) Agentes antiparasitarios
AR097079A1 (es) SALES DE DERIVADOS DE 2-AMINO-1-HIDROXIETIL-8-HIDROXIQUINOLIN-2(1H)-ONA QUE TIENEN ACTIVIDAD ANTAGONISTA DE RECEPTORES MUSCARÍNICOS ASÍ COMO ACTIVIDAD AGONISTA DEL RECEPTOR b2 ADRENÉRGICO
TN2009000160A1 (fr) Derives de pyrazoline utiles comme antagonistes des recepteurs de mineralocorticoides
AR050967A1 (es) Derivados de bencimidazol utiles como moduladores de los receptores androgenicos (sarms)
EA200970705A1 (ru) Новые фармацевтические композиции
EA200970704A1 (ru) ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ, СОДЕРЖАЩИЕ АНТАГОНИСТЫ NK1 РЕЦЕПТОРА И БЛОКАТОРЫ Na КАНАЛОВ
AR061272A1 (es) Antagonistas de cgrp
EA201300436A8 (ru) Совместные кристаллы и соли ингибиторов ccr3
AR078537A1 (es) Derivados heterociclicos de indol ligandos del receptor de estrogenos, composiciones farmaceuticas que los contienen y uso de los mismos para el tratamiento de enfermedades asociadas al sistema nervioso central, osteoporosis, canceres y otras patologias

Legal Events

Date Code Title Description
FB Suspension of granting procedure