PT2735562E - Moduladores de recetores de estrogénio e suas utilizações - Google Patents

Moduladores de recetores de estrogénio e suas utilizações Download PDF

Info

Publication number
PT2735562E
PT2735562E PT141550863T PT14155086T PT2735562E PT 2735562 E PT2735562 E PT 2735562E PT 141550863 T PT141550863 T PT 141550863T PT 14155086 T PT14155086 T PT 14155086T PT 2735562 E PT2735562 E PT 2735562E
Authority
PT
Portugal
Prior art keywords
phenyl
indazol
acrylic acid
fluoro
chloro
Prior art date
Application number
PT141550863T
Other languages
English (en)
Inventor
Steven P Govek
Nicholas D Smith
Mehmet Kahraman
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=PT2735562(E) "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 PT2735562E publication Critical patent/PT2735562E/pt

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

Claims (18)

  1. REIVINDICAÇÕES 1. Composto que tem a estrutura da Fórmula (XII): em que,
    X1 é CH, CR3 ou N; X2 é N, CH ou CR3; Z é -OH ou -OR10; R2 é Ci-C4alquilo, Ci-C4f luoroalquilo, Ci- C4deuteroalquilo, C3-C6cicloalquilo ou -Ci-C4alquileno-W; W é hidroxi, halogéneo, CN, Ci-C4alquilo, Ci-C4haloalquilo, Ci-C4alcoxi, Ci-C4haloalcoxi e C3-C6cicloalquilo; cada R3 é independentemente halogéneo, Ci-C4alquilo ou Ci-C4fluoroalquilo; cada R4 é independentemente halogéneo, -CN, -OR9, S(=0)2R10, Ci-C4alquilo, Ci-C4f luoroalquilo ou Ci-C4heteroalquilo; cada R5 é independentemente halogéneo, -CN, -OR9, S(=0)2R10, Ci-C4alquilo, Ci-C4f luoroalquilo ou Ci-C4heteroalquilo; R6 é H, Ci-C4alquilo ou halogéneo; R7 é H, Ci-C4alquilo ou halogéneo; R9 é H, Ci-C6alquilo, Ci-Cef luoroalquilo ou C3-Cecicloalquilo; R10 é Ci-C6alquilo; m é 0, 1 ou 2; néO, 1, 2, 3 ou 4, e p é 0, 1 ou 2; ou um respetivo sal farmaceuticamente aceitável ou N-óxido.
  2. 2. Composto de acordo com a reivindicação 1, ou um respetivo sal farmaceuticamente aceitável, ou N-óxido, em que: Z é -OH; cada R1 é independentemente halogéneo, Ci-C4alquilo ou Ci-C4fluoroaiquilo; cada R2 é independentemente halogéneo, -CN, -OR3, S(=0)2R4, Ci-C4alquilo, Ci-C4f luoroalquilo ou Ci-C4heteroalquilo; cada R5 é independentemente halogéneo, Ci-C4alquilo ou Ci-C4fluoroalquilo; R6 é H, -CH3, F ou Cl; R7 8 é H, -CH3, F ou Cl; m é 0 ou 1; n é 0, 1 ou 2, e pé 0 ou 1. 1 Composto de acordo com a reivindicação 2, ou um respetivo sal farmaceuticamente aceitável, ou N-óxido, 2 em que:
  3. 3 W é hidroxi, halogéneo, CN, Ci-C4alcoxi ou C3-C6cicloalquilo; 4 R6 é H; 5 Z é -OH; 6 R2 é Ci-C4alquilo, Ci-C4f luoroalquilo, Ci- 7 C4deuteroalquilo, C3-C6cicloalquilo ou -Ci-C4alquileno- 8 W; R7 é Η; m é 0 ou 1; n é 0, 1 ou 2, e p é 0 .
  4. 4. Composto de acordo com a reivindicação 3, ou um respetivo sal farmaceuticamente aceitável, ou N-óxido, em que o composto de Fórmula (XII) tem a estrutura da Fórmula (XIII): R*y\/ 5 i^xl^ H Fórmula (XIII).
  5. 5. Composto de acordo com a reivindicação 3, ou um respetivo sal farmaceuticamente aceitável, ou N-óxido, em que o composto de Fórmula (XII) tem a estrutura da Fórmula (XIV) ou Fórmula (XV): XX ) , X'"' Xj H (R% o Fórmula (XIV) χΧ^ I RV-A/ : Ν' I ,! |! I Η P:5k (R~% 0 Fórmula (XV).
  6. 6. Composto de acordo com qualquer uma das reivindicações 1 até 5, ou um respetivo sal f armaceut icamente aceitável, ou N-óxido, em que: cada R3 é independentemente F, Cl ou -CH3; cada R4 é independentemente halogéneo, -CN, -OH, S(=0)2CH3, -S (=0) 2CH2CH3, -CH3, -CH2CH3, -cf3, - CH2OH, - 0CF3, -OCH3 ou -OCH2CH3; cada R5 é independentemente F, Cl ou -CH3; m é 0 ou 1; n é 0, 1 ou 2, e pé 0 ou 1.
  7. 7. Composto de acordo com a reivindicação 6, ou um respetivo sal farmaceuticamente aceitável, ou N-óxido, em que: R2 é -CH3, -CH2CH3, -CH2CH2CH3, -CH(CH3)2, -CH2CH2CH2CH3, -CH2CH(CH3)2, -CH2F, -CHF2, -CF3, -CH2CF3, -CD3, -CH2CD3, -CD2CD3, ciclopropilo, ciclobutilo, ciclopentilo, ciclo-hexilo, - CH2-W ou -CH2CH2-W; W é hidroxi, F, Cl, -CN, -0CH3, -OCH2CH3, -OCH2CH2CH3, -OCH(CH3)2, ciclopropilo, ciclobutilo, ciclopentilo ou ciclo-hexilo.
  8. 8. Composto de acordo com a reivindicação 7, ou um respetivo sal farmaceuticamente aceitável, ou N-óxido, em que: R2 é -CH2CH3 ou ciclobutilo; cada R4 é independentemente F, Cl, -CN, -OH, -CH3, CH2CH3, -CF3, -CH2OH, -OCF3, -OCH3 ou -OCH2CH3; m é 0 ou 1; n é 0, 1 ou 2, e p é 0 .
  9. 9. Composto de acordo com a reivindicação 1 em que o composto é: 3- (4-((E)-1-(lH-Indazol-5-il)-2-fenilbut-l-en-l-il) fenil)acrilato de (E)-etilo; Ácido (E)-3-(4-((E)-1-(lH-indazol-5-il)-2-fenilbut-l-en-l-il) fenil)acrílico; Ácido (E)-3-(4-((E)-1-(lH-benzo[d] [ 1,2,3]triazol-5-il)-2-fenilbut-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-2-(4-fluorofenil)-1-(lH-indazol-5-il)but-l-en-l-il)fenil)acrílico; Ácido (E)-3-(4-((E)-2-(4-clorofenil)-1-(lH-indazol-5-il)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-1-(lH-indazol-5-il)-2-(3-metoxi-fenil)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-2-(3-(hidroximetil)fenil)-1-(1H-indazol-5-il)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-2-(4-(hidroximetil)fenil)-1-(1H-indazol-5-il)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-2-(2-(hidroximetil)fenil)-1-(1H-indazol-5-il)but-l-en-l-il)fenil)acrílico; Ácido (E)—3— (4—((E)—1—(lH-indazol-5-il)-2-(o-tolil)but-l-en-l-il) fenil)acrílico; Ácido (E)-3-(4-((E)-1-(lH-indazol-5-il)-2-(m-tolil)but-l-en-l-il) fenil)acrílico; Ácido (E)-3-(4-((E)-1-(lH-indazol-5-il)-2-(p-tolil)but-l-en-l-il) fenil)acrílico; Ácido (E)-3- (4- ( (E)-1-(lH-indazol-5-il)-2-(2-metoxi-fenil)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-1-(lH-indazol-5-il)-2-(4-metoxi-fenil)but-l-en-l-il)fenil)acrílico; Ácido ( (E)-3-(4-((E)-2-(2-clorofenil)-1-(lH-indazol-5-il)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4-((E)-2-(3-clorofenil)-1-(lH-indazol-5-il)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-2-(2 — fluorofenil)-1-(lH-indazol-5-il)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-2-(3-fluorofenil)-1-(lH-indazol-5-il)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-2-(2-etilfenil)-1-(lH-indazol-5-il)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4-((E)-1-(lH-indazol-5-il)-2-(2- (trifluorometil)fenil)but-l-en-l-il)fenil) acrílico; Ácido (E)-3- (4-((E)-4-cloro-l-(lH-indazol-5-il) -2- fenilbut-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-2-(2-fluorofenil)-1-(lH-indazol-4-il)but-l-en-l-il)fenil)acrílico; Ácido (E)-3-(4-((E)-2-(2-cianofenil)-1-(lH-indazol-5-il)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-2-(2,4-difluorofenil)-1-(1H- indazol-5-il)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-2-(2-cloro-3-fluorofenil)-1-(1H-indazol-5-il)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-2-ciclopropil-l-(lH-indazol-5-il)-2-fenilvinil)fenil)acrílico; Ácido (E)-3- (4- ( (E)-2-(4-fluoro-2-metilfenil)-1-(1H-indazol-5-il)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-2-(2,6-difluorofenil)-1-(1H- indazol-5-il)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4-((E)-2-(2,6-diclorofenil)-1-(lH-indazol-5-il)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4-((E)-4,4,4-trideutero-l-(lH-indazol-5-il)-2-fenilbut-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-2-(4-fluoro-3-metilfenil)-1-(1H-indazol-5-il)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-2-(5-fluoro-2-metilfenil)-1-(1H-indazol-5-il)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-2-(2,3-difluorofenil)-1-(1H- indazol-5-il)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-2-(2,5-difluorofenil)-1-(1H- indazol-5-il)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-2- (2-cloro-5-fluorofenil)-1-(1H-indazol-5-il)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-2-(2-cloro-6-metilfenil)-1-(1H- indazol-5-il)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-1-(7-cloro-lH-indazol-5-il) -2- fenilbut-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-1-(4-metil-lH-indazol-5-il)-2- fenilbut-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-1-(7-metil-lH-indazol-5-il)-2- fenilbut-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-1-(6-metil-lH-indazol-5-il)-2- fenilbut-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-1-(3-metil-lH-indazol-5-il)-2- fenilbut-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-1-(3-cloro-lH-indazol-5-il)-2- fenilbut-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-2-(4-cloro-2-metilfenil)-1-(1H- indazol-5-il)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-1-(lH-indazol-5-il)-2-fenilprop-1-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-1-(lH-indazol-5-il)-2-fenilpent-1-en-l-il)fenil)acrílico; Ácido (E)-3-(4-((E)-2-(3-cianofenil)-1-(lH-indazol-5-il)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4-((E)-2-(4-cianofenil)-1-(lH-indazol-5-il)but-l-en-l-il)fenil)acrílico; Ácido (E)-3-(4-((E)-4-hidroxi-l-(lH-indazol-5-il)-2-fenilbut-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-1-(lH-indazol-5-il)-4-metoxi-2- fenilbut-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (Z)-1-(lH-indazol-5-il)-3-metoxi-2- fenilprop-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-1-(4-fluoro-lH-indazol-5-il)-2- fenilbut-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-1-(lH-indol-5-il)-2-fenilbut-l-en- Ácido (E)-3- (4- ( (E)-1-(6-cloro-lH-indazol-5-il)-2- fenilbut-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-1-(lH-indazol-5-il)-4-metil-2- fenilpent-l-en-l-il)fenil)acrílico; Ácido (E)-3-(4-((E)-1-(lH-benzo[d][1,2,3]triazol-5-il)-2- (2-cloro-4-fluorofenil)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-1-(4-cloro-lH-indazol-5-il)-2- fenilbut-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-2-ciclopentil-1-(lH-indazol-5-il)-2-fenilvinil)fenil)acrílico; Ácido (E)-3- (4- ( (E)-2-ciclo-hexil-l-(lH-indazol-5-il)-2-fenilvinil)fenil)acrílico; Ácido (E)-3- (4- ( (E)-1-(lH-indazol-5-il)-3-metil-2- fenilbut-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-3-ciclopropil-l-(lH-indazol-5-il)-2-fenilprop-1-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-2-(2-clorofenil)-2-ciclopropil-l-(lH-indazol-5-il)vinil)fenil)acrílico; Ácido (E)-3- (4- ( (E)-1-(6-fluoro-lH-indazol-5-il)-2- fenilbut-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-1-(ΙΗ-benzo[d]imidazol-5-il)-2- fenilbut-l-en-l-il)fenil)acrílico; Ácido (E)-3-(4-((E)-1-(lH-indazol-5-il)-2-fenil-hex-1-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-3-ciclopentil-l-(lH-indazol-5-il)-2-fenilprop-1-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-2-(2-cloro-4-fluorofenil)-1-(4- fluoro-lH-indazol-5-il)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-1-(7-fluoro-lH-indazol-5-il) -2- fenilbut-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-1-(7-fluoro-lH-indol-5-il)-2- fenilbut-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-2-(2-cloro-4-fluorofenil)-1-(1H-indazol-5-il)-4-metilpent-l-en-l-il)fenil)acrílico; Ácido (E)-3-(4-((Z)-3,3-difluoro-1-(lH-indazol-5-il)-2-fenilprop-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-2-(2-cloro-4-fluorofenil)-1-(7- fluoro-lH-indazol-5-il)but-l-en-l-il)fenil) acrílico; Ácido (E)-3- (4- ( (E)-4-fluoro-l-(lH-indazol-5-il)-2- fenilbut-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-4-cloro-2-(2-cloro-4-fluorofenil)-1-(lH-indazol-5-il)but-l-en-l-il)fenil) acrílico; Ácido (E)-3- (4- ( (Z)-3,3,3-trifluoro-1-(lH-indazol-5-il)-2-fenilprop-1-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-1-(4-fluoro-lH-indazol-5-il)-2-(4-fluoro-2-metilfenil)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-2-(4-cloro-2-metilfenil)-1-(4- fluoro-lH-indazol-5-il)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-2-ciclopropil-l-(4-fluoro-lH- indazol-5-il)-2-(4-fluoro-2-metilfenil)vinil)fenil) acrílico; Ácido (E)-3- (4- ( (E)-2-(4-cloro-2-metilfenil)-2- ciclopropil-1-(4-fluoro-lH-indazol-5-il)vinil) fenil) acrílico; Ácido (E)-3- (4-((E)-1-(4-cloro-lH-indazol-5-il)-2-(2-cloro-4-fluorofenil)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (Z)-2-(2-cloro-4-fluorofenil)-3,3- difluoro-1-(lH-indazol-5-il)prop-l-en-l-il)fenil) acrílico; Ácido (E)-3- (4- ( (E)-2-ciclopropil-l-(4-fluoro-lH- indazol-5-il)-2-fenilvinil)fenil) acrílico; Ácido (E)-3-(4-((E)-4-cloro-l-(4-fluoro-lH-indazol-5-il)-2-fenilbut-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-4-cloro-2-(2-cloro-4-fluorofenil)-1- (4-fluoro-lH-indazol-5-il)but-l-en-l-il)fenil) acrílico; Ácido (E)-3- (4-((E)-4-fluoro-2-(4-fluorofenil)-1-(1H-indazol-5-il)but-l-en-l-il)fenil) acrílico; Ácido (E)-3- (4- ( (E)-4-fluoro-l-(4-fluoro-lH-indazol-5-il)-2-fenilbut-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-1-(lH-indazol-5-il)-5-metoxi-2- fenilpent-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4-((E)-1-(lH-indazol-5-il)-6-metoxi-2- fenil-hex-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-2-(2-cloro-4-fluorofenil)-1-(1H-indazol-5-il)-3-metilbut-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4-((E)-1-(lH-indazol-5-il)-2-(3- (trifluorometoxi)fenil)but-l-en-l-il)fenil) acrílico; Ácido (E)-3- (4-((E)-2-ciclobutil-1-(lH-indazol-5-il) -2-fenilvinil)fenil)acrílico; Ácido (E)-3- (4- ( (E)-2-(2-cloro-4-fluorofenil)-2- ciclobutil-1-(lH-indazol-5-il)vinil)fenil)acrílico; Ácido (E)-3- (4- ( (E)-1-(3-fluoro-lH-indazol-5-il)-2- fenilbut-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-2-ciclobutil-1-(3-fluoro-lH- indazol-5-il)-2-fenilvinil)fenil)acrílico; Ácido (E)-3- (4- ( (E)-2-(2-cloro-4-fluorofenil)-1-(3- fluoro-lH-indazol-5-il)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-2-(2-cloro-4-fluorofenil)-2- ciclobutil-1-(3-fluoro-lH-indazol-5-il)vinil)fenil) acrílico; 3- (4 - ( (E)-2 - (4-Fluorofenil)-1-(lH-indazol-5-il)but-l-en-l-il) fenil) acrilato de (E)-etilo; 3-(4-((E)-1-(lH-Indazol-5-il)-2-(2-metoxifenil)but-l-en-l-il ) fenil ) acrilato de (E)-etilo; 3- (4 - ( (E)-1-(lH-Indazol-5-il)-2-(4-metoxifenil)but-l-en-l-il) fenil) acrilato de (E)-etilo; Ácido (E)-3-(4-((E)-1-(lH-indazol-5-il)-2-fenilbut-l-en-l-il)fenil)-2-metilacrílico; Ácido (E)-3- (4- ( (Z)-1-(lH-indazol-5-il)-2-fenilbut-l-en-l-il)-3-metilfenil)acrílico; Ácido (E)-3- (4- ( (E)-1-(lH-indazol-5-il)-2-fenilbut-l-en-l-il)-2-metilfenil)acrílico; Ácido (E)-3- (4-((Z)-1-(lH-indazol-5-il)-2-fenilbut-l-en-l-il)-2-clorofenil)acrílico; Ácido (Z)-3- (4-((E)-1-(lH-indazol-5-il)-2-fenilbut-l-en-l-il)fenil)-2-fluoroacrílico; Ácido (Z)-3- (4- ( (E)-1-(lH-indazol-5-il)-2-fenilbut-l-en-l-il)fenil)-2-cloroacrílico; Ácido (E)-3- (4- ( (Z)-1-(lH-indazol-5-il)-2-fenilbut-l-en-l-il)-3-fluorofenil)acrílico; Ácido (E)-3- (4- ( (Z)-1-(lH-indazol-5-il)-2-fenilbut-l-en-l-il)-2-fluorofenil)acrílico; Ácido (E)-3- (4-((Z)-1-(lH-indazol-5-il)-2-fenilbut-1-en-l-il)-2-(trifluorometil)fenil)acrílico; Ácido (E)-3-(4-((Z)-1-(lH-indazol-5-il)-2-fenilbut-l-en-l-il)-3-metoxifenil)acrílico; Ácido (E)-3-(4-((Z)-1-(lH-indazol-5-il)-2-fenilbut-l-en-l-il)-2-metoxifenil)acrílico; Cloridrato de 3- (4-( (E)-2-(2-cloro-4-fluorofenil)-1-(lH-indazol-5-il)but-l-en-l-il)fenil)acrilato de (E)-etilo; Ácido (E)-3- (4- ( (E)-2-(2-cloro-4-fluorofenil)-1-(1H-indazol-5-il)but-l-en-l-il)fenil)acrílico; 3- (4 - ( (E)-2 - (2,4-Diclorofenil)-1-(lH-indazol-5-il)but-l-en-l-il) fenil) acrilato de (E)-etilo; Ácido (E)-3- (4- ( (E)-2-(2,4-diclorofenil)-1-(lH-indazol-5-il)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-2-(4-cloro-2-(trifluorometil) fenil)-1-(lH-indazol-5-il)but-l-en-l-il) fenil) acrílico; Ácido (E)-3- (4- ( (E)-2-(2-cloro-4-fluorofenil)-2- ciclopropil-1-(lH-indazol-5-il)vinil)fenil)acrílico; Ácido (E)-3- (4- ( (E)-2- (4-fluoro-2-(trifluorometil) fenil)-1-(lH-indazol-5-il)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- (1-(4-Fluoro-lH-indazol-5-il)-2-(4- fluoro-2-(trifluorometil)fenil)butil)fenil)acrílico; Ácido (E)-3-(4-((E)-2-(2,4-diclorofenil)-1-(4-fluoro-lH-indazol-5-il)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-2-(4-cloro-2-(trifluorometil) fenil)-1-(4 — fluoro-lH-indazol-5-il)but-l-en-l-il) fenil) acrílico; Ácido (E)-3- (4-((E)-2-(2-cloro-4-fluorofenil)-4-fluoro-1-(lH-indazol-5-il)but-l-en-l-il)fenil) acrílico; Ácido (E)-3- (4- ( (E)-2-(2-cloro-4-metoxifenil)-1-(1H-indazol-5-il)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4-((E)-2-(2,4-diclorofenil)-4-fluoro-l-(4-fluoro-lH-indazol-5-il)but-l-en-l-il)fenil) acrílico; Ácido (E)-3- (4- ( (E)-2-ciclopropil-2-(2,4-diclorofenil) -1- (4-fluoro-lH-indazol-5-il) vinil)fenil)acrílico; Ácido (E)-3- (4- ( (E)-2-(2-cloro-4-fluorofenil)-2- ciclopropil-1-(4-fluoro-lH-indazol-5-il) vinil)fenil) acrílico; Ácido (E)-3- (4- ( (E)-2-ciclopropil-2-(2,4-diclorofenil)-1-(lH-indazol-5-il)vinil)fenil)acrílico; Ácido (E)-3- (4-((E)-2-(4-cloro-2-metilfenil)-2- ciclopropil-1-(lH-indazol-5-il)vinil)fenil)acrílico; Ácido (E)-3- (4-((E)-1-(lH-indazol-5-il)-2-(2-metil-5-(metilsulfonil)fenil)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-1-(lH-indazol-5-il)-2-(4-metoxi-2-metilfenil)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-2-(2-fluoro-4-metoxifenil)-1-(1H-indazol-5-il)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4-((E)-2-(2-cloro-5-metoxifenil)-1-(1H-indazol-5-il)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-2- (2-fluoro-4-(metilsulfonil) fenil)-1-(lH-indazol-5-il)but-l-en-l-il)fenil)acrílico; Ácido (E)—3— (4— ( (E)-2-(2,4-diclorofenil)-3,3,4,4,4- pentadeutero-1-(lH-indazol-5-il)but-l-en-l-il)fenil) acrílico; Ácido (E)-3- (4- ( (E)-1-(lH-indazol-5-il)-2-(3-(metil-sulfonil)fenil)but-l-en-l-il)fenil)acrílico; Ácido (E)-3-(4-((E)-2-(2,4-diclorofenil)-1-(7-fluoro-lH-indazol-5-il)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-2-(2-cloro-3-metoxifenil)-1-(1H-indazol-5-il)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4-((E)-2-(2,4-diclorofenil)-1-(7-fluoro-lH-indol-5-il)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-2-(2-cloro-4-fluorofenil)-1-(7- fluoro-lH-indol-5-il)but-l-en-l-il)fenil) acrílico; Ácido (E)-3- (4-((E)-2-(2-cloro-4-fluorofenil)- 3,3,4,4,4-pentadeutero-l-(lH-indazol-5-il)but-l-en-l-il) fenil)acrílico; Ácido (E)-3- (4- ( (E)-2-(4-cloro-2-cianofenil)-1-(1H- indazol-5-il)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-2-(2-ciano-4-fluorofenil)-1-(1H-indazol-5-il)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-2-(2-ciano-4-(trifluorometil) fenil)-1-(lH-indazol-5-il)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-2-(2-cloro-4-cianofenil)-1-(1H- indazol-5-il)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-2-(3-ciano-2-metilfenil)-1-(1H- indazol-5-il)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-2-(4-ciano-2-metilfenil)-1-(1H- indazol-5-il)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-2-(5-ciano-2-metilfenil)-1-(1H- indazol-5-il)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-2- (2-ciano-4-metoxifenil)-1-(1H-indazol-5-il)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-2-(3-hidroxifenil)-1-(lH-indazol-5-il)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4-((E)-2-(2-hidroxifenil)-1-(lH-indazol-5-il)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-2-(4-hidroxifenil)-1-(lH-indazol-5-il)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- (1- (lH-indazol-5-il)-2-fenilbut-l-en-1-il)fenil)propanoico; Ácido (E)-3-(4-((E)-1-(lH-indazol-5-il)-2-(4-(2-metoxi-etoxi)fenil)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-1-(lH-indazol-5-il)-2-(4-(3-metoxi-propoxi)fenil)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-1- (lH-indazol-5-il)-2-(3-(2-metoxi-etoxi)fenil)but-l-en-l-il)fenil)acrílico; Ácido (E)-3-(4-((E)-1-(lH-indazol-5-il)-2-(3-(3-metoxi-propoxi)fenil)but-l-en-l-il)fenil)acrílico; Ácido (E)-3-(4-((E)-2-(3-(ciclo-hexiloxi)fenil) -1-(4-fluoro-lH-indazol-5-il)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-2-(3-butoxifenil)-1-(lH-indazol-5-il)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-1-(lH-indazol-5-il)-2-(3-(pentil-oxi)fenil)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-2-(3-(hexiloxi)fenil)-1-(1H- indazol-5-il)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-2-(4-butoxifenil)-1-(lH-indazol-5-il)but-l-en-l-il)fenil)acrílico; Ácido (E)-3-(4-((E)-1-(lH-indazol-5-il)-2-(4-(pentil-oxi)fenil)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-2-(4-(hexiloxi)fenil)-1-(1H- indazol-5-il)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-2-(4-(2-hidroxietoxi)fenil)-1-(1H-indazol-5-il)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-1-(lH-indazol-5-il)-2-(2-(metil-sulfonil)fenil)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-2- (2-clorofenil)-1-(1-metil-lH- indazol-5-il)but-l-en-l-il)fenil)acrílico; Ácido (E)-3-(4-((E)-2-ciclobutil-1-(1-metil-lH-indazol-5-il)-2-fenilvinil)fenil)acrílico; Ácido (E)-3- (4-((E)-2-(2-cloro-4-fluorofenil)-1-(1- metil-lH-indazol-5-il)but-l-en-l-il)fenil)acrílico; Ácido (E)-3- (4- ( (E)-2-(2-cloro-4-fluorofenil)-1-(1- (difluorometil)-lH-indazol-5-il)but-l-en-l-il)fenil) acrílico; ou um respetivo sal farmaceuticamente aceitável ou N-óxido.
  10. 10. Composto de acordo com a reivindicação 1, em que o composto é representado por uma das fórmulas seguintes: ou
    ou um respetivo sal farmaceuticamente aceitável ou N-óxido.
  11. 11. Sal farmaceuticamente aceitável de um composto como reivindicado em qualquer uma das reivindicações 1 até 10 .
  12. 12. Composição farmacêutica compreendendo um composto como reivindicado em qualquer uma das reivindicações 1 até 10, ou um respetivo sal farmaceuticamente aceitável, ou N-óxido e pelo menos um ingrediente inativo farmaceuticamente aceitável.
  13. 13. Composição farmacêutica de acordo com a reivindicação 12, em que a composição farmacêutica é formulada para injeção intravenosa, injeção subcutânea, administração oral ou administração tópica.
  14. 14. Composição farmacêutica de acordo com a reivindicação 15, em que a composição farmacêutica é um comprimido, uma pílula, uma cápsula, um líquido, uma suspensão, um gel, uma dispersão, uma solução, uma emulsão, uma pomada ou uma loção.
  15. 15. Composto de acordo com qualquer uma das reivindicações 1 até 10, ou um respetivo sal farmaceuticamente aceitável, ou N-óxido, para utilização em medicina.
  16. 16. Composto de acordo com qualquer uma das reivindicações 1 até 10, ou um respetivo sal farmaceuticamente aceitável, ou N-óxido, para utilização no tratamento de cancro num mamífero.
  17. 17. Composto de acordo com a reivindicação 16, ou um respetivo sal farmaceuticamente aceitável, ou N-óxido, para utilização no tratamento de cancro da mama, cancro do ovário, cancro endometrial, cancro da próstata ou cancro uterino num mamífero.
  18. 18. Composto de acordo com qualquer uma das reivindicações 1 até 10, ou um respetivo sal farmaceuticamente aceitável, ou N-óxido, para utilização no tratamento de cancro ósseo, cancro da mama, cancro colorretal, cancro endometrial, cancro da próstata, cancro do ovário, cancro uterino, cancro cervical, cancro do pulmão, leiomioma, leiomioma uterino, alcoolismo, enxaqueca, aneurisma aórtico, suscetibilidade a enfarte do miocárdio, esclerose da válvula aórtica, doença cardiovascular, doença das artérias coronárias, hipertensão, trombose venosa profunda, Doença de Grave, artrite, esclerose múltipla, cirrose, hepatite B, doença crónica do fígado, densidade óssea, colestase, hipospadia, obesidade, osteoartrite, osteopenia, osteoporose, doença de Alzheimer, doença de Parkinson, enxaqueca, vertigens, anorexia nervosa, distúrbio de hiperatividade com deficiência de atenção (ADHD), demência, distúrbio depressivo major, psicose, idade de menarca, endometriose ou infertilidade num mamífero. Lisboa,
PT141550863T 2010-09-16 2011-09-15 Moduladores de recetores de estrogénio e suas utilizações PT2735562E (pt)

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
PT2735562E true PT2735562E (pt) 2015-06-18

Family

ID=46599311

Family Applications (1)

Application Number Title Priority Date Filing Date
PT141550863T PT2735562E (pt) 2010-09-16 2011-09-15 Moduladores de recetores de estrogénio e suas utilizações

Country Status (30)

Country Link
US (4) US9399646B2 (pt)
EP (2) EP2616445A4 (pt)
JP (2) JP5903435B2 (pt)
KR (1) KR20130136986A (pt)
CN (1) CN103189361B (pt)
AU (1) AU2011301952B2 (pt)
BR (1) BR112013006395A2 (pt)
CA (1) CA2810094A1 (pt)
CL (1) CL2013000722A1 (pt)
CO (1) CO6680708A2 (pt)
CR (1) CR20130168A (pt)
DK (1) DK2735562T3 (pt)
EA (1) EA023947B1 (pt)
ES (1) ES2535155T3 (pt)
GB (1) GB2483736B (pt)
HK (1) HK1192886A1 (pt)
HR (1) HRP20150433T1 (pt)
HU (1) HUE025746T2 (pt)
IL (1) IL224976A (pt)
MX (1) MX2013002975A (pt)
NZ (1) NZ607795A (pt)
PE (1) PE20140191A1 (pt)
PL (1) PL2735562T3 (pt)
PT (1) PT2735562E (pt)
RS (1) RS54026B1 (pt)
SG (1) SG188551A1 (pt)
SI (1) SI2735562T1 (pt)
TW (1) TWI439268B (pt)
WO (2) WO2012037410A2 (pt)
ZA (1) ZA201301623B (pt)

Families Citing this family (84)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2800673A1 (en) 2010-06-10 2011-12-15 Aragon Pharmaceuticals, Inc. Estrogen receptor modulators and uses thereof
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
US9187460B2 (en) 2011-12-14 2015-11-17 Seragon Pharmaceuticals, Inc. Estrogen receptor modulators and uses thereof
MX2014007198A (es) 2011-12-16 2014-10-13 Olema Pharmaceuticals Inc Compuestos novedosos de benzopirano, composiciones y usos de los mismos.
US9499538B2 (en) * 2012-03-20 2016-11-22 Seragon Pharmaceuticals, Inc. Estrogen receptor modulators and uses thereof
MX2015011132A (es) 2013-03-14 2015-11-30 Seragon Pharmaceuticals Inc Moduladores policiclicos del receptor de estrogenos y sus usos.
BR112015030595A2 (pt) 2013-06-19 2017-07-25 Seragon Pharmaceuticals Inc moduladores de receptor de estrogênio de azetidina e usos dos mesmos
CA2912853A1 (en) 2013-06-19 2014-12-24 Seragon Pharmaceuticals, Inc. Estrogen receptor modulator and uses thereof
AR097617A1 (es) 2013-09-13 2016-04-06 Actelion Pharmaceuticals Ltd Derivados antibacterianos del 2h-indazol
KR20160085915A (ko) * 2013-12-06 2016-07-18 에프. 호프만-라 로슈 아게 국소 진행성 또는 전이성 에스트로겐 수용체 양성 유방암을 치료하기 위한 에스트로겐 수용체 조절자
JP6407288B2 (ja) 2013-12-19 2018-10-17 イドーシア ファーマシューティカルズ リミテッドＩｄｏｒｓｉａ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｌｔｄ 抗菌性１ｈ−インダゾール及び１ｈ−インドール誘導体
MA39741A (fr) * 2014-03-13 2017-01-18 Hoffmann La Roche Combinaisons thérapeutiques avec des modulateurs du récepteur des œstrogènes
CA2941161A1 (en) 2014-03-13 2015-09-17 F.Hoffmann-La Roche Ag Methods and compositions for modulating estrogen receptor mutants
JP2017524009A (ja) 2014-08-11 2017-08-24 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト エストロゲン受容体モジュレーターの結晶形態
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
JP6768711B2 (ja) 2015-05-26 2020-10-14 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト 複素環式エストロゲン受容体モジュレーター及びその使用
EP3981766A1 (en) 2015-05-29 2022-04-13 Eisai R&D Management Co., Ltd. Indazole derivatives useful in the treatment of cancer
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
HUE055321T2 (hu) 2015-10-01 2021-11-29 Olema Pharmaceuticals Inc Tetrahidro-1H-pirido[3,4-b]indol anti-ösztrogén hatóanyagok
JP2018533561A (ja) 2015-10-07 2018-11-15 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト （ｅ）−３−（４−（（ｅ）−２−（２−クロロ−４−フルオロフェニル）−１−（１ｈ−インダゾール−５−イル）ブタ−１−エン−１−イル）フェニル）アクリル酸を調製するためのプロセス
WO2017066633A1 (en) 2015-10-16 2017-04-20 Eisai R&D Management Co., Ltd. Ep4 antagonists
JP6592197B2 (ja) 2015-11-12 2019-10-16 浙江海正薬業股▲ふん▼有限公司Ｚｈｅｊｉａｎｇ Ｈｉｓｕｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌ ＣＯ．，ＬＴＤ． アクリル酸誘導体、製造方法、および医薬としてのその使用
US10118910B2 (en) 2015-12-09 2018-11-06 The Board Of Trustees Of The University Of Illinois Benzothiophene-based selective estrogen receptor downregulators
KR102605762B1 (ko) 2016-02-08 2023-11-27 고완 크롭 프로텍션 리미티드 살균성 조성물
WO2017138068A1 (ja) 2016-02-08 2017-08-17 株式会社エス・ディー・エス バイオテック １，２－ベンゼンジメタノール化合物の製造方法
EA034994B1 (ru) 2016-02-15 2020-04-15 Санофи 6,7-дигидро-5h-бензо[7]аннуленовые производные в качестве модуляторов эстрогеновых рецепторов
KR102111792B1 (ko) * 2016-03-25 2020-05-18 뤄신 바이오테크놀러지 (상하이) 컴퍼니 리미티드 에스트로겐 수용체 하향 조절제로서의 치환된 인돌 화합물
WO2017197055A1 (en) 2016-05-10 2017-11-16 C4 Therapeutics, Inc. Heterocyclic degronimers for target protein degradation
CN109562113A (zh) 2016-05-10 2019-04-02 C4医药公司 用于靶蛋白降解的螺环降解决定子体
WO2017197046A1 (en) 2016-05-10 2017-11-16 C4 Therapeutics, Inc. C3-carbon linked glutarimide degronimers for target protein degradation
CN109789143A (zh) 2016-07-01 2019-05-21 G1治疗公司 基于嘧啶的抗增殖剂
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
BR112019009291A2 (pt) * 2016-11-17 2019-07-30 Sanofi Sa compostos n-(3-fluoropropil)-pirrolidina substituídos, processos para a sua preparação e usos terapêuticos dos mesmos
MA46896A (fr) * 2016-11-24 2019-10-02 Eisai R&D Man Co Ltd Composés d'alcène tétrasubstitués et leur utilisation
WO2018098305A1 (en) * 2016-11-24 2018-05-31 Eisai R&D Management Co., Ltd. Tetrasubstituted alkene compounds and their use for the treatment of breast cancer
JP6346368B1 (ja) * 2016-11-28 2018-06-20 エーザイ・アール・アンド・ディー・マネジメント株式会社 インダゾール誘導体の塩及びその結晶
CN110177554B (zh) 2017-01-06 2023-06-02 G1治疗公司 用于治疗癌症的组合疗法
CN110461853A (zh) 2017-02-10 2019-11-15 G1治疗公司 苯并噻吩雌激素受体调节剂
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
US11083722B2 (en) 2017-03-16 2021-08-10 Eisai R&D Management Co., Ltd. Combination therapies for the treatment of breast cancer
CN110913861B (zh) 2017-06-29 2024-01-09 G1治疗公司 G1t38的形态学形式及其制造方法
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
JP2021503478A (ja) 2017-11-16 2021-02-12 ノバルティス アーゲー 組み合わせ治療
JP2021519337A (ja) 2018-03-26 2021-08-10 シー４ セラピューティクス， インコーポレイテッド Ｉｋａｒｏｓの分解のためのセレブロン結合剤
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
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
MX2021001857A (es) 2018-08-17 2021-10-13 Genentech Inc Star Metodos de diagnostico y terapeuticos para el tratamiento del cancer de mama.
WO2020051235A1 (en) 2018-09-04 2020-03-12 C4 Therapeutics, Inc. Compounds for the degradation of brd9 or mth1
CN112638870A (zh) 2018-09-07 2021-04-09 赛诺菲 用于制备6-(2,4-二氯苯基)-5-[4-[(3s)-1-(3-氟丙基)吡咯烷-3-基]氧基苯基]-8,9-二氢-7h-苯并[7]轮烯-2-甲酸甲酯的方法
US20220017463A1 (en) 2018-11-28 2022-01-20 Luoxin Pharmaceutical (Shanghai) Co., Ltd. Salt Form of Estrogen Receptor Downregulator, Crystalline Form Thereof, and Preparation Method Therefor
CN117430585A (zh) * 2018-12-17 2024-01-23 正大天晴药业集团股份有限公司 雌激素受体拮抗剂
CN113453679A (zh) 2018-12-20 2021-09-28 C4医药公司 靶向蛋白降解
AU2019402189B2 (en) 2018-12-20 2023-04-13 Novartis Ag Dosing regimen and pharmaceutical combination comprising 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives
AU2020222346B2 (en) 2019-02-15 2021-12-09 Novartis Ag Substituted 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives and uses thereof
EA202192019A1 (ru) 2019-02-15 2021-11-02 Новартис Аг Производные 3-(1-оксо-5-(пиперидин-4-ил)изоиндолин-2-ил)пиперидин-2,6-диона и пути их применения
JP2022532918A (ja) 2019-05-20 2022-07-20 ノバルティス アーゲー Ｍｃｌ－１阻害剤抗体－薬物コンジュゲートおよび使用方法
EP3978493A4 (en) 2019-05-24 2023-02-01 Zhejiang Hisun Pharmaceutical Co., Ltd. CRYSTALLINE FORMS OF ACRYLIC ACID DERIVATIVES, METHOD OF MANUFACTURE THEREOF AND USE THEREOF
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
WO2021123996A1 (en) 2019-12-20 2021-06-24 Novartis Ag Uses of anti-tgf-beta antibodies and checkpoint inhibitors for the treatment of proliferative diseases
WO2021260528A1 (en) 2020-06-23 2021-12-30 Novartis Ag Dosing regimen comprising 3-(1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives
CN116134027A (zh) 2020-08-03 2023-05-16 诺华股份有限公司 杂芳基取代的3-(1-氧代异吲哚啉-2-基)哌啶-2,6-二酮衍生物及其用途
WO2022029657A1 (en) * 2020-08-04 2022-02-10 Novmetahealth Co., Ltd. Method for treatment of cytokine release syndrome
WO2022109395A2 (en) 2020-11-23 2022-05-27 Sanofi Panel of er regulated genes for use in monitoring endocrine therapy in breast cancer
EP4251648A2 (en) 2020-11-24 2023-10-04 Novartis AG Anti-cd48 antibodies, antibody drug conjugates, and uses thereof
JP2023553808A (ja) 2020-11-24 2023-12-26 ノバルティス アーゲー Ｍｃｌ－１阻害剤抗体－薬物コンジュゲートおよび使用方法
WO2022169780A1 (en) 2021-02-02 2022-08-11 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
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
CN115960082A (zh) * 2021-10-13 2023-04-14 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
KR20230146812A (ko) * 2022-04-13 2023-10-20 재단법인 대구경북첨단의료산업진흥재단 아릴에텐 유도체를 유효성분으로 포함하는 염증성 장질환 치료용 조성물
WO2023225320A1 (en) 2022-05-20 2023-11-23 Novartis Ag Epha2 bcl-xl inhibitor antibody-drug conjugates and methods of use thereof
WO2023225336A1 (en) 2022-05-20 2023-11-23 Novartis Ag Met bcl-xl inhibitor antibody-drug conjugates and methods of use thereof
WO2024030968A1 (en) 2022-08-03 2024-02-08 Brystol-Myers Squibb Company Compounds for modulating ret protein

Family Cites Families (35)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US410727A (en) 1889-09-10 beigos
US383659A (en) 1888-05-29 Armature for dynamos
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
UA70925C2 (uk) 1997-08-15 2004-11-15 Дюк Юнівесіті Спосіб лікування естрогенстимульованого раку
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
WO2003016270A2 (en) * 2001-08-11 2003-02-27 Bristol-Myers Squibb Pharma Company Selective estrogen receptor modulators
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
WO2006081230A2 (en) 2005-01-26 2006-08-03 Schering Corporation 3-(indazol-5-yl)-(1,2, 4) triazine derivatives and related compounds as protein kinase inhibitors for the treatment of cancer
KR20080045705A (ko) 2005-08-15 2008-05-23 테크니온 리서치 엔드 디벨로프먼트 화운데이션 엘티디. 인쇄가능 재료
WO2007062151A2 (en) * 2005-11-22 2007-05-31 Smithkline Beecham Corporation Chemical compounds
JP2010508358A (ja) 2006-11-01 2010-03-18 ブリストル−マイヤーズ スクイブ カンパニー グルココルチコイド受容体、ＡＰ−１、および／またはＮＦ−κＢ活性の調節剤、並びにその使用
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
WO2009131654A2 (en) 2008-04-21 2009-10-29 North Carolina State University Inhibition and dispersion of bacterial biofilms with imidazole-triazole derivatives
AR074199A1 (es) 2008-11-20 2010-12-29 Glaxosmithkline Llc Compuesto de 6-(4-pirimidinil)-1h-indazol, composiciones farmaceuticas que lo comprenden y su uso para preparar un medicamento util para el tratamiento o disminucion de la gravedad del cancer.
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
EP2616445A2 (en) 2013-07-24
MX2013002975A (es) 2013-04-11
SG188551A1 (en) 2013-04-30
US9868704B2 (en) 2018-01-16
JP2013544761A (ja) 2013-12-19
WO2012037411A2 (en) 2012-03-22
NZ607795A (en) 2015-02-27
ES2535155T3 (es) 2015-05-05
EP2616445A4 (en) 2014-01-15
PE20140191A1 (es) 2014-02-27
CL2013000722A1 (es) 2013-07-26
EP2735562A1 (en) 2014-05-28
HUE025746T2 (en) 2016-04-28
JP2016155832A (ja) 2016-09-01
WO2012037410A9 (en) 2012-05-10
HK1192886A1 (en) 2014-09-05
EP2735562B2 (en) 2023-11-15
PL2735562T3 (pl) 2015-08-31
US8299112B2 (en) 2012-10-30
EA201370066A1 (ru) 2014-01-30
BR112013006395A2 (pt) 2019-09-24
CN103189361A (zh) 2013-07-03
US20130231333A1 (en) 2013-09-05
CR20130168A (es) 2013-08-30
WO2012037411A3 (en) 2012-07-05
AU2011301952A1 (en) 2013-03-21
TWI439268B (zh) 2014-06-01
US20130012561A1 (en) 2013-01-10
AU2011301952B2 (en) 2015-02-19
US9399646B2 (en) 2016-07-26
EP2735562B1 (en) 2015-03-11
US20160297767A1 (en) 2016-10-13
JP5903435B2 (ja) 2016-04-13
WO2012037410A3 (en) 2012-06-28
GB2483736B (en) 2012-08-29
DK2735562T3 (en) 2015-05-11
CN103189361B (zh) 2015-09-30
CA2810094A1 (en) 2012-03-22
US20120071535A1 (en) 2012-03-22
WO2012037410A2 (en) 2012-03-22
GB2483736A (en) 2012-03-21
ZA201301623B (en) 2015-10-28
EA023947B1 (ru) 2016-07-29
TW201216961A (en) 2012-05-01
GB201104288D0 (en) 2011-04-27
US8455534B2 (en) 2013-06-04
IL224976A (en) 2015-08-31
SI2735562T1 (sl) 2015-07-31
CO6680708A2 (es) 2013-05-31
KR20130136986A (ko) 2013-12-13
WO2012037411A9 (en) 2012-05-18
RS54026B1 (en) 2015-10-30
HRP20150433T1 (hr) 2015-07-31

Similar Documents

Publication Publication Date Title
PT2735562E (pt) Moduladores de recetores de estrogénio e suas utilizações
JP2013544761A5 (pt)
JP2015501847A5 (pt)
HRP20211542T1 (hr) Tetrasupstituirani spojevi alkena i njihova uporaba
ES2360726T3 (es) Agonistas del receptor de niacina, composiciones que contienen dichos compuestos y procedimientos de tratamiento.
JP2020529405A5 (pt)
CA2477601A1 (en) 5-phenylthiazole derivatives and use as pi3 kinase inhibitors
RU2010112967A (ru) Соединения, моделирующие внутриклеточный кальций
Kumar et al. Developments in synthesis of the anti-inflammatory drug, celecoxib: a review
JP2011520806A (ja) Ｃｃｒ１アンタゴニストとしてのピラゾール化合物
RU2008116313A (ru) Диарилминсодержащие соединения, композиции и их примеение в качестве модуляторов рецепторов с-кit
WO2014125426A1 (en) Trisubstituted heterocyclic derivatives as ror gamma modulators
ES2426345T3 (es) Compuesto unidos en posición 1-amino
JP2013508438A (ja) （１，１，１，３，３，３−ヘキサフルオロ−２−ヒドロキシプロパン−２−イル）フェニル誘導体、それらの医薬組成物およびアテローム性動脈硬化症の処置のためのそれらの使用
US9434699B2 (en) Iodine(III)-mediated radiofluorination
CN1221524C (zh) 治疗用的二苯基醚化合物
ES2335305T3 (es) Derivados de pirrolidina como antagonistas del receptor h3 de histamina.
CA2819215C (en) Pyrazole compounds having therapeutic effect on multiple myeloma
US20190062304A1 (en) Tetrahydroisoquinolines as prmt5 inhibitors
WO2009131127A1 (ja) ５－ヒドロキシピリミジン－４－カルボキサミド化合物
ES2665421T3 (es) Compuestos de pirimidina y su uso como moduladores de la gamma secretasa
AR064002A1 (es) Quinazolinas sustituidas
KR101181692B1 (ko) 피리미디닐이속사졸 유도체
US8772499B2 (en) TRPV3 modulators
Keung et al. Structure-based optimization of 1H-imidazole-2-carboxamides as Axl kinase inhibitors utilizing a Mer mutant surrogate