[go: up one dir, main page]

PE20140191A1 - Moduladores de receptores de estrogenos y usos de los mismos - Google Patents

Moduladores de receptores de estrogenos y usos de los mismos

Info

Publication number
PE20140191A1
PE20140191A1 PE2013000500A PE2013000500A PE20140191A1 PE 20140191 A1 PE20140191 A1 PE 20140191A1 PE 2013000500 A PE2013000500 A PE 2013000500A PE 2013000500 A PE2013000500 A PE 2013000500A PE 20140191 A1 PE20140191 A1 PE 20140191A1
Authority
PE
Peru
Prior art keywords
phenyl
modulators
compounds
indazol
rent
Prior art date
Application number
PE2013000500A
Other languages
English (en)
Inventor
Nicholas Smith
Mehmet Kahraman
Steven Govek
Johnny Y Nagasawa
Andiliy G Lai
Jackaline D Julien
Mark R Herbert
Celine Bonnefous
Karensa L Douglas
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=46599311&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20140191(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Seragon Pharmaceuticals Inc filed Critical Seragon Pharmaceuticals Inc
Publication of PE20140191A1 publication Critical patent/PE20140191A1/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
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/7056—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • A61K31/7072—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7076—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7076—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid
    • A61K31/708—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid having oxo groups directly attached to the purine ring system, e.g. guanosine, guanylic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7088—Compounds having three or more nucleosides or nucleotides
    • A61K31/7105—Natural ribonucleic acids, i.e. containing only riboses attached to adenine, guanine, cytosine or uracil and having 3'-5' phosphodiester links
    • 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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • 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
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular 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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32—Alcohol-abuse
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • A61P31/12—Antivirals
    • 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
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • 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
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
    • C07C215/02—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C215/04—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated
    • C07C215/06—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and acyclic
    • C07C215/10—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and acyclic with one amino group and at least two hydroxy groups bound to the carbon skeleton
    • 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
    • C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D215/20—Oxygen atoms
    • C07D215/22—Oxygen atoms attached in position 2 or 4
    • C07D215/227—Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems 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 carbon atoms of the nitrogen-containing ring
    • C07D217/24—Oxygen atoms
    • 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
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/04—1,3-Oxazines; Hydrogenated 1,3-oxazines
    • C07D265/12—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems
    • C07D265/14—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D265/18—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring with hetero atoms 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
    • C07D277/68—Benzothiazoles 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
    • C07D279/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
    • C07D279/10—1,4-Thiazines; Hydrogenated 1,4-thiazines
    • C07D279/14—1,4-Thiazines; Hydrogenated 1,4-thiazines condensed with carbocyclic rings or ring systems
    • C07D279/16—1,4-Thiazines; Hydrogenated 1,4-thiazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • 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
    • C07D401/02—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
    • C07D401/12—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 chain containing hetero atoms as chain links
    • 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
    • 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
    • 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
    • C07D413/10—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 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
    • C07D417/10—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 aromatic rings
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Psychiatry (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Reproductive Health (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Biochemistry (AREA)
  • Hospice & Palliative Care (AREA)
  • Addiction (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)

Abstract

SE REFIERE A COMPUESTOS HETEROCICLICOS DE FORMULA (I) DONDE EL ANILLO A ES INDANILO, NAFTILO, HETEROARILO MONOCICLICO DE 5 O 6 MIEMBROS, ENTRE OTROS; LOS ANILLOS B Y C SON CADA UNO FENILO, INDANILO, NAFTILO, HETEROCICLO BICICLICO DE 8 A 10 MIEMBROS; ENTRE OTROS; R1 ES Y, X-ALQUILEN(C1-C6)-Y, ALQUILEN(C1-C6)-Y, ENTRE OTROS, EN DONDE X ES O, S, S(=O), ENTRE OTROS; Y ES TETRAZOLILO, PIPERIDINILO, PIRROLIDINILO, ENTRE OTROS; R2 ES HALOGENO, CN, NO2, ALQUILO(C1-C6), ENTRE OTROS; R3, R4 Y R5 SON CADA UNO H, HALOGENO, OH, ALQUENILO(C2-C6), ENTRE OTROS; m, n Y p SON CADA UNO DE 0 A 4. SON COMPUESTOS PREFERIDOS: 3-(4-((E)-1-(1H-INDAZOL-5-IL)-2-FENILBUT-1-EN-1-IL)FENIL)ACRILATO DE (E)-ETILO; ACIDO (E)-3-(4-((E)-1-(1H-INDAZOL-5-IL)-2-FENILBUT-1-EN-1-IL)FENIL)ACRILICO; ACIDO (E)-3-(4-((E)-1-(1H-BENZO[d][1,2,3]TRIAZOL-5-IL)-2-FENILBUT-1-EN-1-IL)FENIL)ACRILICO; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON MODULADORES DE RECEPTORES DE ESTROGENOS SIENDO UTILES EN EL TRATAMIENTO DE CANCER DE HUESO, CANCER DE MAMA, LEIOMIOMA, ARTERIOPATIA CORONARIA
PE2013000500A 2010-09-16 2011-09-15 Moduladores de receptores de estrogenos y usos de los mismos PE20140191A1 (es)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US38365910P 2010-09-16 2010-09-16
US41072710P 2010-11-05 2010-11-05
US201161446967P 2011-02-25 2011-02-25
GB1104288.4A GB2483736B (en) 2010-09-16 2011-03-15 Estrogen receptor modulators and uses thereof

Publications (1)

Publication Number Publication Date
PE20140191A1 true PE20140191A1 (es) 2014-02-27

Family

ID=46599311

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2013000500A PE20140191A1 (es) 2010-09-16 2011-09-15 Moduladores de receptores de estrogenos y usos de los mismos

Country Status (30)

Country Link
US (4) US9399646B2 (es)
EP (2) EP2735562B2 (es)
JP (2) JP5903435B2 (es)
KR (1) KR20130136986A (es)
CN (1) CN103189361B (es)
AU (1) AU2011301952B2 (es)
BR (1) BR112013006395A2 (es)
CA (1) CA2810094A1 (es)
CL (1) CL2013000722A1 (es)
CO (1) CO6680708A2 (es)
CR (1) CR20130168A (es)
DK (1) DK2735562T3 (es)
EA (1) EA023947B1 (es)
ES (1) ES2535155T3 (es)
GB (1) GB2483736B (es)
HR (1) HRP20150433T1 (es)
HU (1) HUE025746T2 (es)
IL (1) IL224976A (es)
MX (1) MX2013002975A (es)
NZ (1) NZ607795A (es)
PE (1) PE20140191A1 (es)
PH (1) PH12013500481A1 (es)
PL (1) PL2735562T3 (es)
PT (1) PT2735562E (es)
RS (1) RS54026B1 (es)
SG (1) SG188551A1 (es)
SI (1) SI2735562T1 (es)
TW (1) TWI439268B (es)
WO (2) WO2012037411A2 (es)
ZA (1) ZA201301623B (es)

Families Citing this family (104)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2012014431A (es) 2010-06-10 2013-02-26 Aragon Pharmaceuticals Inc Modulares del receptor de estrogenos y usos de los mismos.
GB2483736B (en) 2010-09-16 2012-08-29 Aragon Pharmaceuticals Inc Estrogen receptor modulators and uses thereof
WO2013056178A2 (en) 2011-10-14 2013-04-18 Foundation Medicine, Inc. Novel estrogen receptor mutations and uses thereof
MX357496B (es) 2011-12-14 2018-07-11 Seragon Pharmaceuticals Inc Moduladores del receptor de estrógenos fluorados y sus usos.
PE20150099A1 (es) 2011-12-16 2015-01-30 Olema Pharmaceuticals Inc Compuestos novedosos de benzopirano, composiciones y usos de los mismos
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
CA2915534A1 (en) 2013-06-19 2014-12-24 Seragon Pharmaceuticals, Inc. Azetidine estrogen receptor modulators and uses thereof
EA031077B1 (ru) 2013-06-19 2018-11-30 Серагон Фармасьютикалз, Инк. Модулятор рецептора эстрогена и его применения
AR097617A1 (es) 2013-09-13 2016-04-06 Actelion Pharmaceuticals Ltd Derivados antibacterianos del 2h-indazol
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
TR201807881T4 (tr) 2013-12-19 2018-06-21 Idorsia Pharmaceuticals Ltd Antibakteriyel 1h-ındazol ve 1h-ındol türevleri.
EP3116497A2 (en) * 2014-03-13 2017-01-18 F. Hoffmann-La Roche AG Therapeutic combinations with estrogen receptor modulators
WO2015136017A1 (en) 2014-03-13 2015-09-17 F. Hoffmann-La Roche Ag Methods and compositions for modulating estrogen receptor mutants
EP3180316A1 (en) 2014-08-11 2017-06-21 F. Hoffmann-La Roche AG Crystalline forms of an estrogen receptor modulator
WO2016024350A1 (ja) 2014-08-13 2016-02-18 株式会社エス・ディー・エス バイオテック 縮合１１員環化合物及びそれらを含有する農園芸用殺菌剤
JP6359940B2 (ja) * 2014-10-14 2018-07-18 国立大学法人 名古屋工業大学 ジフルオロメチルアセチレン化合物類及びその製造方法
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
KR101771794B1 (ko) 2015-08-04 2017-08-25 경북대학교 산학협력단 트리아졸로-아릴아크릴로나이트라일 유도체 및 이의 용도
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
IL310489A (en) 2015-10-01 2024-03-01 Olema Pharmaceuticals Inc TETRAHYDRO-1H-PYRIDO[3,4-b]INDOLE ANTI-ESTROGENIC DRUGS AND COMPOSITIONS COMPRISING SAME FOR USE IN TREATING CANCER
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
CA3002144C (en) 2015-10-16 2024-01-23 Eisai R&D Management Co., Ltd. Ep4 antagonists
US10519148B2 (en) 2015-11-12 2019-12-31 Zhejiang Hisun Pharmaceutical Co., Ltd. Acrylic acid derivative, preparation method and use in medicine thereof
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
CN114702411A (zh) 2016-02-08 2022-07-05 高文作物保护公司 1,2-苯二甲醇化合物的制造方法
AU2016392652B2 (en) 2016-02-08 2021-01-21 Gowan Company, L.L.C. Fungicidal Composition
PE20181893A1 (es) 2016-02-15 2018-12-11 Sanofi Sa Nuevos compuestos de 6,7-dihidro-5h-benzo[7]anuleno sustituidos, procesos para su preparacion y usos terapeuticos de los mismos
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
EP3455219A4 (en) 2016-05-10 2019-12-18 C4 Therapeutics, Inc. AMINE-RELATED C3-GLUTARIMIDE DEGRONIMERS FOR TARGET PROTEIN REDUCTION
EP3455218A4 (en) 2016-05-10 2019-12-18 C4 Therapeutics, Inc. C3 CARBON-BASED GLUTARIMIDE DEGRONIMERS FOR TARGET PROTEIN REDUCTION
EP4491236A3 (en) 2016-05-10 2025-04-02 C4 Therapeutics, Inc. Heterocyclic degronimers for target protein degradation
WO2017197036A1 (en) 2016-05-10 2017-11-16 C4 Therapeutics, Inc. Spirocyclic degronimers for target protein degradation
KR20190025943A (ko) 2016-07-01 2019-03-12 쥐원 쎄라퓨틱스, 인크. 피리미딘-기재 항증식제
CN107973780B (zh) * 2016-10-21 2020-10-09 四川科伦博泰生物医药股份有限公司 一种取代的烯烃类化合物及其制备方法和用途
WO2018081168A2 (en) 2016-10-24 2018-05-03 The Board Of Trustees Of The University Of Illinois Benzothiophene-based selective mixed estrogen receptor downregulators
CN106632144B (zh) * 2016-10-31 2019-02-26 浙江省医学科学院 一种环丙烷类化合物及其制备方法和应用
JP6946430B2 (ja) * 2016-11-17 2021-10-06 サノフイＳａｎｏｆｉ 新規の置換ｎ−（３−フルオロプロピル）−ピロリジン化合物、それを製造するための方法、およびその治療的使用
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
JP2019535781A (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
CN109963854B (zh) 2017-03-16 2022-04-12 江苏恒瑞医药股份有限公司 杂芳基并[4,3-c]嘧啶-5-胺类衍生物、其制备方法及其在医药上的应用
CN110636862A (zh) * 2017-03-16 2019-12-31 卫材 R&D 管理有限公司 用于治疗乳腺癌的组合疗法
CN118440096A (zh) 2017-06-20 2024-08-06 C4医药公司 用于蛋白降解的n/o-连接的降解决定子和降解决定子体
WO2019006393A1 (en) 2017-06-29 2019-01-03 G1 Therapeutics, Inc. Morphic forms of git38 and methods of manufacture thereof
EP3434272A1 (en) 2017-07-25 2019-01-30 Sanofi Combination comprising palbociclib and 6-(2,4-dichlorophenyl)-5-[4-[(3s)-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7h-benzo[7]annulene-2-carboxylic acid
US11034653B2 (en) 2017-09-25 2021-06-15 Luoxin Pharmaceutical (Shanghai) Co., Ltd. Crystal form of estrogen receptor inhibitor and preparation method therefor
AU2018368731A1 (en) 2017-11-16 2020-05-14 Novartis Ag Combination therapies
KR20210018199A (ko) 2018-03-26 2021-02-17 씨4 테라퓨틱스, 인코포레이티드 이카로스의 분해를 위한 세레블론 결합제
CN108558838B (zh) * 2018-04-20 2021-04-20 苏州凌科特新材料有限公司 一种雌激素受体调节剂中间体的生产方法
CN108503648B (zh) * 2018-04-27 2020-04-14 安徽医科大学 苯乙烯基吡唑并嘧啶类化合物、药物组合物及制备方法与用途
US20190375732A1 (en) 2018-05-14 2019-12-12 David Hung Anti-cancer nuclear hormone receptor-targeting compounds
WO2019225552A1 (en) * 2018-05-22 2019-11-28 Eisai R&D Management Co., Ltd. Salts of indazole derivative and crystals thereof
US10487057B1 (en) * 2018-07-05 2019-11-26 Landos Biopharma, Inc. NLRX1 ligands
AR116109A1 (es) 2018-07-10 2021-03-31 Novartis Ag Derivados de 3-(5-amino-1-oxoisoindolin-2-il)piperidina-2,6-diona y usos de los mismos
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
EP3846800A4 (en) 2018-09-04 2022-08-24 C4 Therapeutics, Inc. Compounds for the degradation of brd9 or mth1
AU2019335542A1 (en) 2018-09-07 2021-04-01 Sanofi Process for the preparation of methyl 6-(2,4-dichlorophenyl)-5-(4-((3s)-1-(3-fluoropropyl)pyrrolidin-3-yl)oxyphenyl)-8,9-dihydro-7H-benzo(7)annulene-2-carboxylate
US12098127B2 (en) 2018-11-28 2024-09-24 Luoxin Pharmaceutical (Shanghai) Co., Ltd. Salt form of estrogen receptor downregulator, crystalline form thereof, and preparation method therefor
MY208271A (en) * 2018-12-17 2025-04-29 Chia Tai Tianqing Pharmaceutical Group Co Ltd Estrogen receptor antagonist
CN120698985A (zh) 2018-12-20 2025-09-26 C4医药公司 靶向蛋白降解
WO2020128972A1 (en) 2018-12-20 2020-06-25 Novartis Ag Dosing regimen and pharmaceutical combination comprising 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives
ES2982474T3 (es) 2019-02-15 2024-10-16 Novartis Ag Derivados de 3-(1-oxoisoindolin-2-il)piperidin-1,6-diona sustituidos y usos de estos
ES3032659T3 (en) 2019-02-15 2025-07-23 Novartis Ag 3-(1-oxo-5-(piperidin-4-yl)isoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof
KR20210152515A (ko) 2019-04-12 2021-12-15 씨4 테라퓨틱스, 인코포레이티드 이카로스 및 아이올로스의 트리시클릭 분해제
KR20220008869A (ko) 2019-05-14 2022-01-21 누베이션 바이오 인크. 항암 핵 호르몬 수용체-표적화 화합물
UY38700A (es) 2019-05-20 2020-12-31 Novartis Ag Conjugados de anticuerpo-fármaco inhibidores de mcl-1 y sus métodos de uso
US20220220107A1 (en) 2019-05-24 2022-07-14 Zhejiang Hisun Pharmaceutical Co., Ltd. Crystal forms of acrylic acid derivatives, preparation method therefor and use thereof
US12325696B2 (en) * 2019-06-19 2025-06-10 Jiangsu Hengrui Medicine Co., Ltd. Indazole derivative, preparation method therefor, and pharmaceutical application thereof
MX2022000279A (es) 2019-07-07 2022-02-03 Olema Pharmaceuticals Inc Regimenes de antagonistas del receptor de estrogeno.
CN110452177A (zh) * 2019-09-02 2019-11-15 南通大学 一种5-溴-4-氟-1h-吲唑的合成方法
MX2022007759A (es) 2019-12-20 2022-07-19 Novartis Ag Combinacion del anticuerpo anti tim-3 mbg453 y anticuerpo anti tgf-beta nis793, con o sin decitabina o el anticuerpo anti pd-1 spartalizumab, para el tratamiento de mielofibrosis y sindrome mielodisplasico.
MX2022007659A (es) 2019-12-20 2022-07-19 C4 Therapeutics Inc Compuestos de isoindolinona e indazol para la degradacion del receptor del factor de crecimiento epidermico (egfr).
TW202146007A (zh) 2020-02-27 2021-12-16 法商賽諾菲公司 包含阿培利司（ａｌｐｅｌｉｓｉｂ）與６－（２，４－二氯苯基）－５－［４－［（３ｓ）－１－（３－氟丙基）吡咯啶－３－基］氧苯基］－８，９－二氫－７ｈ－苯并［７］輪烯－２－羧酸之組合
AU2021231898A1 (en) 2020-03-05 2022-10-27 C4 Therapeutics, Inc. Compounds for targeted degradation of BRD9
AU2021273744A1 (en) 2020-05-19 2022-12-08 Pharmacosmos Holding A/S Cyclin-dependent kinase inhibiting compounds for the treatment of medical disorders
MX2022015852A (es) 2020-06-23 2023-01-24 Novartis Ag Regimen de dosificacion que comprende derivados de 3-(1-oxoisoindolin-2-il)piperidina-2,6-diona.
EP4188549A1 (en) 2020-08-03 2023-06-07 Novartis AG Heteroaryl substituted 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof
CN116113409A (zh) * 2020-08-04 2023-05-12 诺麦塔制药有限公司 细胞因子释放综合征的治疗方法
JP2023538517A (ja) 2020-08-05 2023-09-08 シーフォー セラピューティクス， インコーポレイテッド Ｒｅｔの標的分解のための化合物
CN116437913A (zh) 2020-09-23 2023-07-14 艾其林医药公司 用于治疗补体介导的病症的药物化合物
JP2023551192A (ja) 2020-11-23 2023-12-07 サノフイ 乳がんにおける内分泌療法のモニタリングに使用するためのｅｒ制御遺伝子のパネル
PE20240225A1 (es) 2020-11-24 2024-02-16 Novartis Ag Anticuerpos anti-cd48, conjugados de anticuerpo-farmaco, y usos de los mismos
US20240042051A1 (en) 2020-11-24 2024-02-08 Francesca Rocchetti Mcl-1 inhibitor antibody-drug conjugates and methods of use
AU2022218128A1 (en) 2021-02-02 2023-08-17 Les Laboratoires Servier Selective bcl-xl protac compounds and methods of use
TW202304979A (zh) 2021-04-07 2023-02-01 瑞士商諾華公司 抗ＴＧＦβ抗體及其他治療劑用於治療增殖性疾病之用途
AR125874A1 (es) 2021-05-18 2023-08-23 Novartis Ag Terapias de combinación
MX2023014059A (es) 2021-06-08 2024-03-12 C4 Therapeutics Inc Terapeuticos para la degradacion de una proteina quiinasa de serina/ treonina mutante.
CN117440950A (zh) * 2021-06-27 2024-01-23 北京盛诺基医药科技股份有限公司 一种ERα受体共价结合拮抗剂
CN115960082B (zh) * 2021-10-13 2024-06-07 长春金赛药业有限责任公司 一种四取代的烯烃化合物、其制备方法及其在医药上的应用
KR102729791B1 (ko) * 2022-04-13 2024-11-14 재단법인 대구경북첨단의료산업진흥재단 아릴에텐 유도체를 유효성분으로 포함하는 염증성 장질환 치료용 조성물
EP4525925A1 (en) 2022-05-20 2025-03-26 Novartis AG Epha2 bcl-xl inhibitor antibody-drug conjugates and methods of use thereof
US20250339547A1 (en) 2022-05-20 2025-11-06 Novartis Ag Met bcl-xl inhibitor antibody-drug conjugates and methods of use thereof
JP2025525917A (ja) 2022-08-03 2025-08-07 ブリストル－マイヤーズ スクイブ カンパニー Ｒｅｔタンパク質を調節するための化合物
CN120569388A (zh) 2022-11-04 2025-08-29 百时美施贵宝公司 Ret-ldd蛋白降解剂
EP4611900A1 (en) 2022-11-04 2025-09-10 Bristol-Myers Squibb Company Ret-ldd protein inhibitors
WO2024189481A1 (en) 2023-03-10 2024-09-19 Novartis Ag Panras inhibitor antibody-drug conjugates and methods of use thereof
WO2025006753A2 (en) 2023-06-30 2025-01-02 Merck Patent Gmbh Heterobifunctional compounds for the degradation of kras protein
WO2025111450A1 (en) 2023-11-22 2025-05-30 Les Laboratoires Servier Anti-cd74 antibody-drug conjugates and methods of use thereof
WO2025215536A1 (en) 2024-04-10 2025-10-16 Novartis Ag Macrocyclic panras inhibitors for the treatment of cancer

Family Cites Families (35)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US383659A (en) 1888-05-29 Armature for dynamos
US410727A (en) 1889-09-10 beigos
FR1390978A (fr) * 1963-11-20 1965-03-05 Ind Chimique Sa Procédé de préparation de l'alpha-(thiényl-2) 4-hydroxystilbène et de quelques dérivés et produits obtenus
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
US4755386A (en) 1986-01-22 1988-07-05 Schering Corporation Buccal formulation
US5739136A (en) 1989-10-17 1998-04-14 Ellinwood, Jr.; Everett H. Intraoral dosing method of administering medicaments
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
DE19807760A1 (de) 1997-02-27 1998-09-03 Fuji Electric Co Ltd Elektrofotografischer Fotoleiter
ATE411016T1 (de) 1997-08-15 2008-10-15 Univ Duke Verfahren zur prophylaxis oder behandlung von östrogen-abhängigen krankheiten
DE19801598C2 (de) 1998-01-17 2000-05-11 Aventis Res & Tech Gmbh & Co Katalytische Synthese von N-alkylierten Anilinen aus Olefinen und Anilinen
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
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
US20080255089A1 (en) * 2005-11-22 2008-10-16 Smithkline Beecham Corporation Triphenylethylene Compounds Useful as Selective Estrogen Receptor Modulators
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
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

Also Published As

Publication number Publication date
HUE025746T2 (en) 2016-04-28
DK2735562T3 (en) 2015-05-11
CL2013000722A1 (es) 2013-07-26
RS54026B1 (sr) 2015-10-30
BR112013006395A2 (pt) 2019-09-24
EA023947B1 (ru) 2016-07-29
CN103189361A (zh) 2013-07-03
SG188551A1 (en) 2013-04-30
US9399646B2 (en) 2016-07-26
JP2013544761A (ja) 2013-12-19
KR20130136986A (ko) 2013-12-13
US20160297767A1 (en) 2016-10-13
CN103189361B (zh) 2015-09-30
WO2012037410A2 (en) 2012-03-22
EA201370066A1 (ru) 2014-01-30
JP5903435B2 (ja) 2016-04-13
EP2616445A2 (en) 2013-07-24
EP2735562B1 (en) 2015-03-11
EP2616445A4 (en) 2014-01-15
WO2012037410A3 (en) 2012-06-28
ZA201301623B (en) 2015-10-28
ES2535155T3 (es) 2015-05-05
JP2016155832A (ja) 2016-09-01
MX2013002975A (es) 2013-04-11
AU2011301952B2 (en) 2015-02-19
HK1192886A1 (en) 2014-09-05
AU2011301952A1 (en) 2013-03-21
SI2735562T1 (sl) 2015-07-31
US20120071535A1 (en) 2012-03-22
WO2012037411A9 (en) 2012-05-18
US20130012561A1 (en) 2013-01-10
GB2483736B (en) 2012-08-29
WO2012037410A9 (en) 2012-05-10
CR20130168A (es) 2013-08-30
US8455534B2 (en) 2013-06-04
EP2735562B2 (en) 2023-11-15
HRP20150433T1 (hr) 2015-07-31
CA2810094A1 (en) 2012-03-22
TWI439268B (zh) 2014-06-01
GB201104288D0 (en) 2011-04-27
WO2012037411A3 (en) 2012-07-05
US8299112B2 (en) 2012-10-30
US20130231333A1 (en) 2013-09-05
WO2012037411A2 (en) 2012-03-22
GB2483736A (en) 2012-03-21
PH12013500481A1 (en) 2013-05-27
PT2735562E (pt) 2015-06-18
US9868704B2 (en) 2018-01-16
NZ607795A (en) 2015-02-27
CO6680708A2 (es) 2013-05-31
TW201216961A (en) 2012-05-01
EP2735562A1 (en) 2014-05-28
PL2735562T3 (pl) 2015-08-31
IL224976A (en) 2015-08-31

Similar Documents

Publication Publication Date Title
PE20140191A1 (es) Moduladores de receptores de estrogenos y usos de los mismos
PE20090276A1 (es) Compuestos derivados de imidazoquinolina como moduladores de tlr7
PE20090890A1 (es) Compuestos derivados de 1-(2,3-dihidrobenzo[1,4]dioxin-2-ilmetil)azaciclos como antagonistas del suptipo adrenoreceptor alfa2c
PE20142019A1 (es) Nuevos derivados de acidos indaniloxidihidrobenzofuranilaceticos y sus usos como agonistas del receptor gpr40
PE20091621A1 (es) Derivados de amina como moduladores de la actividad de tlr y composiciones que los contienen
PE20121282A1 (es) Antagonistas de espiro-oxindol de mdm2
PE20141203A1 (es) Benzilindazoles sustituidos para uso como inhibidores de la quinasa bub1 en el tratamiento de enfermedades hiperproliferativas
AR059957A1 (es) DERIVADOS DE ESPIROINDOLINONA, MÉTODOS PARA SU PREPARACIoN, UNA COMPOSICIoN FARMACÉUTICA QUE LOS CONTIENE Y SU USO EN LA FABRICACIoN DE MEDICAMENTOS PARA EL TRATAMIENTO DEL CÁNCER.
PE20141075A1 (es) 4-aril-n-fenil-1,3,5-triazin-2-aminas que contienen un grupo sulfoximina
PE20161399A1 (es) Compuestos de aril y heteroaril eter como moduladores de ror gamma
PE20090622A1 (es) Nuevos derivados de bencimidazol sustituido
PE20121474A1 (es) Nuevos compuestos de espiropiperidina
PE20140207A1 (es) Composiciones y metodos para modular el fxr
PE20121500A1 (es) 2-amino-5,5-difluor-5,6-dihidro-4h-oxazinas como inhibidores de bace 1 y/o bace 2
PE20160844A1 (es) Compuestos triciclicos como agentes anticancerigenos
PE20131143A1 (es) Nuevas aminopirazoloquinazolinas
PE20141682A1 (es) Derivados de (4-fenilimidazol-2-il) etilamina utiles como moduladores de canal de sodio
PE20130149A1 (es) Derivados de la cromenona con actividad anti-tumoral
PE20091173A1 (es) Derivados de heteroarilo como antagonistas de receptor de orexina
PE20140868A1 (es) Antagonistas trpm8 y su uso en tratamientos
PE20141943A1 (es) Antagonistas de trpv4
PE20160664A1 (es) Compuestos heteroaromaticos y su uso como ligandos d1 de dopamina
PE20080065A1 (es) Compuestos derivados de bencimidazol como moduladores del receptor vainilloide vr1
PE20110875A1 (es) Derivados de isoindol como inhibidores de bace
PE20090160A1 (es) COMPUESTOS AMINO-5-[4-(DIFLUOROMETOXI)FENIL SUSTITUIDO]-5-FENILIMIDAZOLONA COMO INHIBIDORES DE ß-SECRETASA

Legal Events

Date Code Title Description
FC Refusal