[go: up one dir, main page]

PE20142461A1 - Moduladores del receptor de estrogeno y sus usos - Google Patents

Moduladores del receptor de estrogeno y sus usos

Info

Publication number
PE20142461A1
PE20142461A1 PE2014001451A PE2014001451A PE20142461A1 PE 20142461 A1 PE20142461 A1 PE 20142461A1 PE 2014001451 A PE2014001451 A PE 2014001451A PE 2014001451 A PE2014001451 A PE 2014001451A PE 20142461 A1 PE20142461 A1 PE 20142461A1
Authority
PE
Peru
Prior art keywords
halogen
estrogen receptor
receptor modulators
phenyl
ring
Prior art date
Application number
PE2014001451A
Other languages
English (en)
Inventor
Nicholas D Smith
Steven P Govek
Mehmet Kahraman
Jackaline D Julien
Johnny Y Nagasawa
Karensa L Douglas
Celine Bonnefous
Andiliy G Lai
Original Assignee
Seragon Pharmaceuticals 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 Seragon Pharmaceuticals Inc filed Critical Seragon Pharmaceuticals Inc
Publication of PE20142461A1 publication Critical patent/PE20142461A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • 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
    • A61P25/06—Antimigraine agents
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • 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
    • 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
    • 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
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00—General protective or antinoxious agents
    • A61P39/02—Antidotes
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • 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
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/32—Oxygen atoms
    • C07D209/34—Oxygen atoms in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/44—Iso-indoles; Hydrogenated iso-indoles
    • C07D209/46—Iso-indoles; Hydrogenated iso-indoles with an oxygen atom in position 1
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/16—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms condensed with carbocyclic rings or ring systems
    • C07D249/18—Benzotriazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/52—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
    • C07D263/54—Benzoxazoles; Hydrogenated benzoxazoles
    • C07D263/58—Benzoxazoles; Hydrogenated benzoxazoles 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 in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62—Benzothiazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62—Benzothiazoles
    • C07D277/64—Benzothiazoles with only hydrocarbon or substituted hydrocarbon radicals attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
    • 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
    • C07D401/14—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 three or more hetero rings
    • 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
    • C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • 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
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D405/06—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 linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D405/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • C07D409/06—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 linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D409/10—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 linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Landscapes

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

Abstract

REFERIDA A UN COMPUESTO DE FORMULA (III), DONDEEL ANILLO B ES FENILO, NAFTILO, ENTRE OTROS; EL ANILLO C ES FENILO, HETEROARILO MONOCICLICO DE 5 MIEMBROS, ENTRE OTROS; R1 ES C(=O)-Z, ENTRE OTROS; Z ES OH, NHOH, ENTRE OTROS; Ra ES H, HALOGENO, CN, OH, ENTRE OTROS; Rb ES H, HALOGENO, OH, CN, ENTRE OTROS; Rc ES H, HALOGENO, CN, OH, ENTRE OTROS; R4 ES H, HALOGENO, CN, OH, ENTRE OTROS; R5 Y R6 SON H, ALQUILO C1-C4 O HALOGENO; m Y n SON 0, 1, 2 O 3; p ES 0, 1 O 2; r ES 1, 2, 3 O 4. DICHOS COMPUESTOS SON MODULADORES DEL RECEPTOR DE ESTROGENO
PE2014001451A 2012-03-20 2013-03-14 Moduladores del receptor de estrogeno y sus usos PE20142461A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201261613442P 2012-03-20 2012-03-20

Publications (1)

Publication Number Publication Date
PE20142461A1 true PE20142461A1 (es) 2015-02-05

Family

ID=49223229

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2014001451A PE20142461A1 (es) 2012-03-20 2013-03-14 Moduladores del receptor de estrogeno y sus usos

Country Status (17)

Country Link
US (1) US9499538B2 (es)
EP (1) EP2828243B1 (es)
JP (1) JP6154887B2 (es)
KR (1) KR20140138296A (es)
CN (1) CN104220426B (es)
AU (1) AU2013235499A1 (es)
CA (1) CA2866891A1 (es)
CO (1) CO7170179A2 (es)
CR (1) CR20140479A (es)
EA (1) EA201491530A1 (es)
IL (1) IL234487A0 (es)
MX (1) MX2014011217A (es)
NZ (1) NZ630124A (es)
PE (1) PE20142461A1 (es)
PH (1) PH12014502095A1 (es)
SG (1) SG11201405918XA (es)
WO (1) WO2013142266A1 (es)

Families Citing this family (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EA201491530A1 (ru) 2012-03-20 2015-07-30 Серагон Фармасьютикалс, Инк. Модуляторы рецепторов эстрогенов и их применение
RU2015138964A (ru) 2013-03-14 2017-04-18 Серагон Фармасьютикалз, Инк. Полициклические модуляторы рецептора эстрогена и их применения
DK2988743T3 (da) 2013-03-15 2021-03-01 Epigen Biosciences Inc Heterocykliske forbindelser, der kan anvendes til behandling af sygdom
EA031077B1 (ru) 2013-06-19 2018-11-30 Серагон Фармасьютикалз, Инк. Модулятор рецептора эстрогена и его применения
CA2915534A1 (en) 2013-06-19 2014-12-24 Seragon Pharmaceuticals, Inc. Azetidine estrogen receptor modulators and uses thereof
WO2015082990A1 (en) 2013-12-06 2015-06-11 Seragon Pharmaceuticals, Inc. Estrogen receptor modulator for the treatment of locally advanced or metastatic estrogen receptor positive breast cancer
WO2015136017A1 (en) * 2014-03-13 2015-09-17 F. Hoffmann-La Roche Ag Methods and compositions for modulating estrogen receptor mutants
EP3116497A2 (en) 2014-03-13 2017-01-18 F. Hoffmann-La Roche AG Therapeutic combinations with estrogen receptor modulators
EP3180316A1 (en) 2014-08-11 2017-06-21 F. Hoffmann-La Roche AG Crystalline forms of an estrogen receptor modulator
US10053451B2 (en) 2015-05-26 2018-08-21 Genentech, Inc. Heterocyclic estrogen receptor modulators and uses thereof
BR112017025546B1 (pt) 2015-05-29 2023-02-14 Eisai R&D Management Co., Ltd Composto, composição farmacêutica compreendendo o referido composto e seus usos
CN105061316B (zh) * 2015-07-17 2017-12-22 苏州大学 稠环类化合物、制备方法和用途
CN106518768B (zh) * 2015-09-15 2021-07-02 江苏恒瑞医药股份有限公司 丙烯酸类衍生物、其制备方法及其在医药上的应用
WO2017060326A1 (en) * 2015-10-07 2017-04-13 F. Hoffmann-La Roche Ag Process for the preparation of (e)-3-(4-((e)-2-(2-chloro-4-fluorophenyl)-1-(1h-indazol-5-yl)but-1-en-1-yl)phenyl)acrylic acid
HRP20221462T1 (hr) 2015-12-09 2023-01-20 The Board Of Trustees Of The University Of Illinois Selektivni nishodni regulatori receptora estrogena na bazi benzotiofena
WO2017162206A1 (zh) * 2016-03-25 2017-09-28 南京明德新药研发股份有限公司 作为雌激素受体降解剂的吲哚并取代哌啶类化合物
IL285318B (en) 2016-04-01 2022-09-01 Kalyra Pharmaceuticals Inc Estrogen receptor modulators
CN113912586B (zh) 2016-08-31 2023-04-07 江苏恒瑞医药股份有限公司 氧代吡啶酰胺类衍生物、其制备方法及其在医药上的应用
WO2018081168A2 (en) 2016-10-24 2018-05-03 The Board Of Trustees Of The University Of Illinois Benzothiophene-based selective mixed estrogen receptor downregulators
JP2019535778A (ja) * 2016-11-24 2019-12-12 エーザイ・アール・アンド・ディー・マネジメント株式会社 四置換アルケン化合物及び乳がんを治療するためのその使用
ES2954879T3 (es) 2016-11-28 2023-11-27 Eisai R&D Man Co Ltd Sales de derivado de indazol y cristales de las mismas
EP3565558B1 (en) 2017-01-06 2023-12-06 G1 Therapeutics, Inc. Combination therapy with a serd compound and a cdk4/6 inhibitor for the treatment of cancer
KR20190117582A (ko) 2017-02-10 2019-10-16 쥐원 쎄라퓨틱스, 인크. 벤조티오펜 에스트로겐 수용체 조정제
CN108976187B (zh) * 2017-06-02 2021-11-26 上海青东生物科技有限公司 一种取代苯并呋喃衍生物及其制备与在制备抗肿瘤药物中的应用
WO2019225552A1 (en) * 2018-05-22 2019-11-28 Eisai R&D Management Co., Ltd. Salts of indazole derivative and crystals thereof
CN113490850B (zh) 2018-08-17 2024-12-06 基因泰克公司 用于治疗乳腺癌的诊断和治疗方法
MY208271A (en) * 2018-12-17 2025-04-29 Chia Tai Tianqing Pharmaceutical Group Co Ltd Estrogen receptor antagonist
US12325696B2 (en) * 2019-06-19 2025-06-10 Jiangsu Hengrui Medicine Co., Ltd. Indazole derivative, preparation method therefor, and pharmaceutical application thereof
BR112022002138A2 (pt) 2019-08-06 2022-04-19 Recurium Ip Holdings Llc Moduladores do receptor de estrogênio para tratamento de mutantes
JP2024502270A (ja) 2020-12-23 2024-01-18 リキュリウム アイピー ホールディングス リミテッド ライアビリティー カンパニー エストロゲン受容体調節薬
CN115745895A (zh) * 2021-11-13 2023-03-07 温州奥洋科技有限公司 一种紫外线吸收剂二苯嘧啶乙烯的结构与合成路线
CN116239562B (zh) * 2021-12-07 2024-12-31 江苏师范大学 一种以苯并呋喃酮为原料合成盐酸多塞平的方法

Family Cites Families (42)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0002097B1 (en) 1977-08-22 1981-08-05 Imperial Chemical Industries Plc Triphenylalkene derivatives, process for their preparation and pharmaceutical compositions containing them
US4229447A (en) 1979-06-04 1980-10-21 American Home Products Corporation Intraoral methods of using benzodiazepines
US4596795A (en) 1984-04-25 1986-06-24 The United States Of America As Represented By The Secretary, Dept. Of Health & Human Services Administration of sex hormones in the form of hydrophilic cyclodextrin derivatives
JPH0778017B2 (ja) 1985-12-28 1995-08-23 住友製薬株式会社 パルス的かつ持続放出性製剤
US4755386A (en) 1986-01-22 1988-07-05 Schering Corporation Buccal formulation
US5052558A (en) 1987-12-23 1991-10-01 Entravision, Inc. Packaged pharmaceutical product
US5033252A (en) 1987-12-23 1991-07-23 Entravision, Inc. Method of packaging and sterilizing a pharmaceutical product
US5739136A (en) 1989-10-17 1998-04-14 Ellinwood, Jr.; Everett H. Intraoral dosing method of administering medicaments
US5017381A (en) 1990-05-02 1991-05-21 Alza Corporation Multi-unit pulsatile delivery system
US5229135A (en) 1991-11-22 1993-07-20 Prographarm Laboratories Sustained release diltiazem formulation
US5323907A (en) 1992-06-23 1994-06-28 Multi-Comp, Inc. Child resistant package assembly for dispensing pharmaceutical medications
JP3409366B2 (ja) 1993-06-18 2003-05-26 東洋インキ製造株式会社 有機エレクトロルミネッセンス素子
US5681835A (en) 1994-04-25 1997-10-28 Glaxo Wellcome Inc. Non-steroidal ligands for the estrogen receptor
US5837284A (en) 1995-12-04 1998-11-17 Mehta; Atul M. Delivery of multiple doses of medications
DE19807760A1 (de) 1997-02-27 1998-09-03 Fuji Electric Co Ltd Elektrofotografischer Fotoleiter
US5840329A (en) 1997-05-15 1998-11-24 Bioadvances Llc Pulsatile drug delivery system
ATE411016T1 (de) 1997-08-15 2008-10-15 Univ Duke Verfahren zur prophylaxis oder behandlung von östrogen-abhängigen krankheiten
DE19801597C2 (de) 1998-01-17 2001-05-03 Aventis Res & Tech Gmbh & Co Basenkatalysierte Synthese von 1-Aryl-4-(arylethyl)piperazinen aus aromatischen Olefinen und 1-Arylpiperazinen
DE19801598C2 (de) 1998-01-17 2000-05-11 Aventis Res & Tech Gmbh & Co Katalytische Synthese von N-alkylierten Anilinen aus Olefinen und Anilinen
TW593256B (en) 1999-11-16 2004-06-21 Hormos Medical Oy Ltd Triphenylalkene derivatives and their use as selective estrogen receptor modulators
GB9929988D0 (en) 1999-12-17 2000-02-09 Celltech Therapeutics Ltd Chemical compounds
US6528681B2 (en) * 2000-04-05 2003-03-04 Bristol-Meyers Squibb Pharma Company Halogenated triphenylethylene derivatives as selective estrogen receptor modulators
JP2005528320A (ja) 2001-08-11 2005-09-22 ブリストル−マイヤーズ・スクイブ・ファーマ・カンパニー 選択的なエストロゲン受容体モジュレーター
JP4562523B2 (ja) 2002-06-06 2010-10-13 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー トロンボポエチン疑似体
ATE399775T1 (de) * 2003-10-08 2008-07-15 Smithkline Beecham Corp Triphenylethyleneverbindungen als selektive modulatoren des östrogenrezeptors
DE102004028862A1 (de) * 2004-06-15 2005-12-29 Merck Patent Gmbh 3-Aminoindazole
US20070292545A1 (en) 2005-10-18 2007-12-20 Aaron Monte Anti-infective agents and methods of use
JP4804480B2 (ja) * 2005-01-26 2011-11-02 シェーリング コーポレイション 癌の処置のためのプロテインキナーゼインヒビターとしての、３−（インダゾール−５−イル）−（１，２，４）トリアジン誘導体、および関連する化合物
JP2009504872A (ja) 2005-08-15 2009-02-05 テクニオン リサーチ アンド ディベロップメント ファウンデーション リミテッド 印刷可能な材料
EP2099767A1 (en) 2006-11-01 2009-09-16 Brystol-Myers Squibb Company Modulators of glucocorticoid receptor, ap-1, and/or nf- b activity and use thereof
JP2008156313A (ja) 2006-12-26 2008-07-10 Fyuuensu:Kk アミロイド疾患の治療およびモニタリングのための薬剤
GB0704407D0 (en) 2007-03-07 2007-04-18 Glaxo Group Ltd Compounds
DE102007049451A1 (de) * 2007-10-16 2009-04-23 Merck Patent Gmbh 5-Cyano-thienopyridine
JP5223362B2 (ja) 2008-02-07 2013-06-26 コニカミノルタビジネステクノロジーズ株式会社 光電変換素子及び太陽電池
US7897631B2 (en) 2008-04-21 2011-03-01 North Carolina State University Inhibition and dispersion of bacterial biofilms with imidazole-triazole derivatives
EP2362775B1 (en) 2008-11-20 2015-08-05 GlaxoSmithKline LLC Chemical compounds
US20110294668A1 (en) 2008-12-08 2011-12-01 North Carolina State University Inhibition and dispersion of biofilms in plants with imidazole-triazole derivatives
WO2010107474A1 (en) 2009-03-16 2010-09-23 The Research Foundation Of State University Of New York Antiestrogens for breast cancer therapy
WO2010144959A1 (en) 2009-06-18 2010-12-23 Fibrotech Therapeutics Pty Ltd Analogues of anti-fibrotic agents
GB2483736B (en) 2010-09-16 2012-08-29 Aragon Pharmaceuticals Inc Estrogen receptor modulators and uses thereof
EA201491530A1 (ru) 2012-03-20 2015-07-30 Серагон Фармасьютикалс, Инк. Модуляторы рецепторов эстрогенов и их применение
JP6126562B2 (ja) * 2014-08-27 2017-05-10 三星ダイヤモンド工業株式会社 光ファイバ装置

Also Published As

Publication number Publication date
CR20140479A (es) 2014-12-01
NZ630124A (en) 2016-01-29
SG11201405918XA (en) 2014-10-30
CN104220426A (zh) 2014-12-17
EA201491530A1 (ru) 2015-07-30
HK1202535A1 (en) 2015-10-02
IL234487A0 (en) 2014-11-02
US20150105403A1 (en) 2015-04-16
CN104220426B (zh) 2017-03-01
CA2866891A1 (en) 2013-09-26
EP2828243A1 (en) 2015-01-28
US9499538B2 (en) 2016-11-22
AU2013235499A8 (en) 2014-10-02
JP2015514072A (ja) 2015-05-18
EP2828243B1 (en) 2018-10-17
KR20140138296A (ko) 2014-12-03
EP2828243A4 (en) 2015-10-28
MX2014011217A (es) 2015-03-10
CO7170179A2 (es) 2015-01-28
PH12014502095A1 (en) 2014-11-24
WO2013142266A1 (en) 2013-09-26
AU2013235499A1 (en) 2014-09-25
JP6154887B2 (ja) 2017-06-28

Similar Documents

Publication Publication Date Title
PE20142461A1 (es) Moduladores del receptor de estrogeno y sus usos
PE20160122A1 (es) Compuestos nobles y composiciones para la inhibicion de fasn
MX2018002402A (es) Compuestos de heteroarilo o arilo biciclicos fusionados como moduladores de la quinasa 4 asociada al receptor de la interleucina 1 (irak4).
PH12015501005A1 (en) Heteroaryl substituted pyridil compounds useful as kinase modulators
MX2017006266A (es) Compuestos de heteroarilo como inhibidores de cinasas asociadas al receptor de interleucina 1(irak) y sus usos.
EA201590292A1 (ru) Соединения, которые являются sip-модулирующими агентами и/или atx-модулирующими агентами
MX373436B (es) Compuesto peptidico.
EA201600091A1 (ru) 4-членные кольцевые карбоксамиды, применяемые в качестве нематоцидов
JOP20190211A1 (ar) ببتيد منشط لمستقبل gip
AR098912A1 (es) Inhibidores de syk
EA201591503A1 (ru) Производные нафтиридина, полезные в качестве антагонистов альфа-v-бета-6 интегрина
MX368615B (es) Derivados bicíclicos como inhibidores de la autotaxina (atx) que son inhibidores de la producción de ácido lisofosfatídico (lpa) y el uso de los mismos.
PE20130155A1 (es) Derivados de ariletinilo
WO2016105165A3 (ko) 유기 발광 화합물 및 이를 이용한 유기 전계 발광 소자
AR101815A1 (es) Compuestos y composiciones como inhibidores de quinasa
TN2018000020A1 (en) Colony stimulating factor-1 receptor (csf-1r) inhibitors.
EA201591805A1 (ru) Оксабицикло [2.2.2] кислоты - модуляторы gpr120
MX2016015923A (es) Compuestos de pirazol y su uso como bloqueadores de canales de calcio tipo t.
MX2015010106A (es) Moduladores de la proteina activadora de 5-lipoxigenasa.
AR084173A1 (es) Derivados oxazolil-metileter como agonistas del receptor alx
EA201591815A1 (ru) Бицикло [2.2.2] кислоты - модуляторы gpr120
EA201492255A1 (ru) Феноксиэтилпиперидиновые соединения
MX374637B (es) Moduladores de ror gamma (ror?).
CL2017000616A1 (es) Compuestos triazólicos como bloqueadores de canales de calcio tipo t
MX2015016400A (es) Nuevos compuestos de 3,4-dihidro-2h-isoquinolin-1-ona y 2,3-dihidro-isoindol-1-ona.

Legal Events

Date Code Title Description
FD Application declared void or lapsed