AR087273A1 - 3-(fluorovinil)pirazoles y su uso - Google Patents
3-(fluorovinil)pirazoles y su usoInfo
- Publication number
- AR087273A1 AR087273A1 ARP120102653A ARP120102653A AR087273A1 AR 087273 A1 AR087273 A1 AR 087273A1 AR P120102653 A ARP120102653 A AR P120102653A AR P120102653 A ARP120102653 A AR P120102653A AR 087273 A1 AR087273 A1 AR 087273A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- fluorine
- cycloalkyl
- series
- alkoxy
- Prior art date
- Legal status (The legal status 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 status listed.)
- Pending
Links
- 229910052731 fluorine Inorganic materials 0.000 abstract 7
- 239000011737 fluorine Substances 0.000 abstract 7
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 6
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 6
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 6
- 229910052739 hydrogen Inorganic materials 0.000 abstract 6
- 239000001257 hydrogen Substances 0.000 abstract 6
- -1 hydroxy, hydroxymethyl Chemical group 0.000 abstract 5
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 4
- 125000001153 fluoro group Chemical group F* 0.000 abstract 4
- 125000000623 heterocyclic group Chemical group 0.000 abstract 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 4
- 238000011282 treatment Methods 0.000 abstract 4
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 abstract 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 3
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 abstract 3
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 3
- 230000006806 disease prevention Effects 0.000 abstract 3
- 229910052757 nitrogen Inorganic materials 0.000 abstract 3
- 125000001424 substituent group Chemical group 0.000 abstract 3
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 3
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 229940079593 drug Drugs 0.000 abstract 2
- 239000003814 drug Substances 0.000 abstract 2
- 150000002221 fluorine Chemical class 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- 150000002431 hydrogen Chemical class 0.000 abstract 2
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 239000012453 solvate Substances 0.000 abstract 2
- 229910052717 sulfur Inorganic materials 0.000 abstract 2
- 125000004769 (C1-C4) alkylsulfonyl group Chemical group 0.000 abstract 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 abstract 1
- 206010021143 Hypoxia Diseases 0.000 abstract 1
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical group C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 abstract 1
- 230000006978 adaptation Effects 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 1
- 125000005196 alkyl carbonyloxy group Chemical group 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 230000002491 angiogenic effect Effects 0.000 abstract 1
- 229910052801 chlorine Inorganic materials 0.000 abstract 1
- 239000000460 chlorine Substances 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000000000 cycloalkoxy group Chemical group 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 230000003463 hyperproliferative effect Effects 0.000 abstract 1
- 230000007954 hypoxia Effects 0.000 abstract 1
- 238000002483 medication Methods 0.000 abstract 1
- 230000002503 metabolic effect Effects 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 1
- 125000004043 oxo group Chemical group O=* 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 125000004076 pyridyl group Chemical group 0.000 abstract 1
- 238000009097 single-agent therapy Methods 0.000 abstract 1
- 230000001225 therapeutic effect Effects 0.000 abstract 1
- 125000004665 trialkylsilyl group Chemical group 0.000 abstract 1
Classifications
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- 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
-
- 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
- A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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- 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
- A61K31/695—Silicon compounds
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
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- 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
- A61P35/00—Antineoplastic agents
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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- 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
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- 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
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
- C07F7/02—Silicon compounds
- C07F7/08—Compounds having one or more C—Si linkages
- C07F7/0803—Compounds with Si-C or Si-Si linkages
- C07F7/081—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te
- C07F7/0812—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te comprising a heterocyclic ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
- C07F7/02—Silicon compounds
- C07F7/08—Compounds having one or more C—Si linkages
- C07F7/10—Compounds having one or more C—Si linkages containing nitrogen having a Si-N linkage
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Urology & Nephrology (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Procedimientos para su preparación, a su uso para el tratamiento y/o la prevención de enfermedades así como a su uso para la preparación de medicamentos para el tratamiento y/o la prevención de enfermedades, especialmente para el tratamiento y/o la prevención de enfermedades hiperproliferativas y angiogénicas así como aquellas enfermedades que se producen debido a una adaptación metabólica a estados de hipoxia. Tales tratamientos puede realizarse como monoterapia o también en combinación con otros medicamentos u otras medidas terapéuticas.Reivindicación 1: Compuesto de la fórmula (1) en la que uno de los dos restos R1A y R1B representa flúor y el otro representa hidrógeno; Ar con el sustituyente R2 representa un anillo fenilo o piridilo del grupo de fórmulas (2), en la que * marca el punto de unión con el grupo CH2 adyacente; R2 representa hidrógeno o un sustituyente seleccionado de la serie halógeno, ciano, alquilo C1-6, alquenilo C2-6, cicloalquilo C3-6, alcoxi C1-6, cicloalcoxi C3-6, alcoxicarbonilo C1-4, alquilsulfonilo C1-4, -NR5R6 y -C(=O)-NR5R6, pudiendo alquilo C1-6 a su vez estar hasta trisustituido con flúor así como hasta disustituido, de manera igual o diferente, con un resto seleccionado de la serie hidroxi, alcoxi C1-4, alquilcarboniloxi C1-4 y cicloalquilo C3-6 y los grupos cicloalquilo mencionados a su vez puedan estar hasta disustituidos, de manera igual o diferente, con un resto seleccionado de la serie flúor, alquilo C1-4, trifluorometilo, hidroxi, hidroximetilo, alcoxi C1-4 y alquilcarboniloxi C1-4, y en la que R5 y R6 independientemente entre sí significan hidrógeno, alquilo C1-6 o cicloalquilo C3-6 o R5 y R6 están enlazados entre sí y junto con el átomo de nitrógeno al que están unidos forman un heterociclo de 4 - 6 miembros, que puede contener otro heteroátomo de la serie N, O, S o S(O)2 y que puede estar hasta disustituido, de manera igual o diferente, con un resto seleccionado de la serie flúor, ciano, hidroxi, alcoxi C1-4, oxo, alquilo C1-4 y cicloalquilo C3-6, pudiendo alquilo C1-4 a su vez estar hasta trisustituido con flúor; R3 representa un sustituyente seleccionado de la serie halógeno, ciano, pentafluorotio, tri-alquilsililo C1-4, alquilo C1-6, -NR7R8, -OR8, -SR8, -S(O)2-R8, cicloalquilo C3-6 y heterociclilo de 4 a 6 miembros, pudiendo alquilo C1-6 a su vez estar sustituido con un resto seleccionado de la serie amino, -NR7R8, hidroxi, -OR8, cicloalquilo C3-6 y heterociclilo de 4 a 6 miembros así como hasta sustituido seis veces con flúor y los grupos cicloalquilo y heterociclilo mencionados a su vez pueden estar hasta disustituidos, de manera igual o diferente, con un resto seleccionado de la serie flúor, alquilo C1-4, trifluorometilo, hidroxi y alcoxi C1-4, y en la que R7 significa hidrógeno o alquilo C1-4 y R8 significa alquilo C1-6 o cicloalquilo C3-6, pudiendo alquilo C1-6, a su vez estar sustituido con un resto seleccionado de la serie hidroxi, alcoxi C1-4, -NR9R10 y -C(=O)-NR9R10 así como hasta trisustituido con flúor, en el que R9 y R10 independientemente entre sí representan hidrógeno o alquilo C1-4 o están enlazados entre sí y junto con el átomo de nitrógeno, al que están unidos, forman un anillo de pirrolidina, piperidina o morfolina; y A representa N o C-R4 en el que R4 significa hidrógeno, flúor, cloro, ciano, metilo, trifluorometilo o metoxi; así como sus sales, solvatos y solvatos de las sales.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP11174843 | 2011-07-21 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR087273A1 true AR087273A1 (es) | 2014-03-12 |
Family
ID=46514386
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP120102653A Pending AR087273A1 (es) | 2011-07-21 | 2012-07-20 | 3-(fluorovinil)pirazoles y su uso |
Country Status (6)
Country | Link |
---|---|
US (1) | US20130150325A1 (es) |
EP (1) | EP2734505A1 (es) |
AR (1) | AR087273A1 (es) |
CA (1) | CA2842352A1 (es) |
UY (1) | UY34200A (es) |
WO (1) | WO2013011033A1 (es) |
Families Citing this family (15)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CA2919397C (en) | 2013-09-09 | 2021-05-18 | Peloton Therapeutics, Inc. | Aryl ethers as hif-2.alpha. inhibitors for the treatment of cancer |
EP3083639B1 (en) | 2013-12-16 | 2019-05-29 | Peloton Therapeutics, Inc. | Cyclic sulfone and sulfoximine analogs and uses thereof |
NZ727818A (en) | 2014-06-03 | 2020-06-26 | Idorsia Pharmaceuticals Ltd | Pyrazole compounds and their use as t-type calcium channel blockers |
WO2016145045A1 (en) | 2015-03-11 | 2016-09-15 | Peloton Therapeutics, Inc. | Compositions for use in treating glioblastoma |
WO2016144826A1 (en) | 2015-03-11 | 2016-09-15 | Peloton Therapeutics, Inc. | Substituted pyridines and uses thereof |
EP3267792A4 (en) | 2015-03-11 | 2018-09-26 | Peloton Therapeutics, Inc. | Compositions for use in treating pulmonary arterial hypertension |
US10807948B2 (en) | 2015-03-11 | 2020-10-20 | Peloton Therapeutics, Inc. | Aromatic compounds and uses thereof |
WO2016168510A1 (en) | 2015-04-17 | 2016-10-20 | Peloton Therapeutics, Inc. | Combination therapy of a hif-2-alpha inhibitor and an immunotherapeutic agent and uses thereof |
US9796697B2 (en) | 2015-06-12 | 2017-10-24 | Peloton Therapeutics, Inc. | Tricyclic inhibitors of HIF-2-alpha and uses thereof |
MX2019007117A (es) | 2016-12-16 | 2019-09-16 | Idorsia Pharmaceuticals Ltd | Combinacion farmaceutica que comprende un bloqueador del canal de calcio de tipo t. |
MA47409A (fr) | 2017-02-06 | 2019-12-11 | Idorsia Pharmaceuticals Ltd | Nouveau procédé de synthèse de 1-aryl-1-trifluorométhylcyclopropanes |
KR20220118425A (ko) | 2019-12-20 | 2022-08-25 | 누에볼루션 에이/에스 | 핵 수용체 활성 화합물 |
CN111007182B (zh) * | 2019-12-30 | 2022-03-25 | 山东华安新材料有限公司 | 一种气相色谱法测定2,2-二氟乙醇中杂质的方法 |
US20230365589A1 (en) | 2020-09-18 | 2023-11-16 | Sumitomo Pharma Co., Ltd. | Novel amine derivatives |
CN116183772B (zh) * | 2023-03-03 | 2023-09-15 | 华夏生生药业(北京)有限公司 | 一种原料药中致突变杂质检测方法 |
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CN1466572A (zh) | 2000-07-28 | 2004-01-07 | ס����ҩ��ʽ���� | 吡咯衍生物 |
CA2424540A1 (en) | 2000-10-05 | 2003-04-02 | Bayer Aktiengesellschaft | Propionic acid derivatives with ppar-alpha activating properties |
US6759428B2 (en) | 2001-12-04 | 2004-07-06 | Roche Palo Alto Llc | Indole nitriles |
US7192976B2 (en) * | 2002-12-21 | 2007-03-20 | Angion Biomedica Corporation | Small molecule modulators of hepatocyte growth factor (scatter factor) activity |
AU2004275694B2 (en) | 2003-06-30 | 2008-03-06 | Bizbiotech Co., Ltd. | Compounds, compositions and methods |
WO2007065010A2 (en) | 2005-12-02 | 2007-06-07 | Hif Bio, Inc. | Anti-angiogenesis compounds |
US7745477B2 (en) | 2006-02-07 | 2010-06-29 | Hoffman-La Roche Inc. | Heteroaryl and benzyl amide compounds |
TW200831091A (en) | 2006-12-20 | 2008-08-01 | Astrazeneca Ab | New compounds |
JP2010518080A (ja) | 2007-02-08 | 2010-05-27 | メルク・シャープ・エンド・ドーム・コーポレイション | 治療薬 |
CN101765596B (zh) | 2007-05-18 | 2015-04-29 | 拜耳知识产权有限责任公司 | 用于治疗过增生症状和与血管生成有关疾病的缺氧诱导因子(hif)抑制剂 |
JP2011516442A (ja) | 2008-04-04 | 2011-05-26 | ビオマリン アイジーエー リミテッド | 筋ジストロフィーを治療するための化合物 |
EP2356112A1 (de) | 2008-11-14 | 2011-08-17 | Bayer Schering Pharma Aktiengesellschaft | Heteroaromatische verbindungen zur verwendung als hif-inhibitoren |
CA2743536A1 (en) | 2008-11-14 | 2010-05-20 | Bayer Schering Pharma Aktiengesellschaft | Heterocyclically substituted aryl compounds as hif inhibitors |
DE102008057344A1 (de) | 2008-11-14 | 2010-05-20 | Bayer Schering Pharma Aktiengesellschaft | Aminoalkyl-substituierte Aryl-Verbindungen und ihre Verwendung |
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- 2012-07-13 UY UY0001034200A patent/UY34200A/es not_active Application Discontinuation
- 2012-07-17 EP EP12735557.6A patent/EP2734505A1/de not_active Withdrawn
- 2012-07-17 WO PCT/EP2012/064021 patent/WO2013011033A1/de active Application Filing
- 2012-07-17 US US13/551,175 patent/US20130150325A1/en not_active Abandoned
- 2012-07-17 CA CA2842352A patent/CA2842352A1/en not_active Abandoned
- 2012-07-20 AR ARP120102653A patent/AR087273A1/es active Pending
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CA2842352A1 (en) | 2013-01-24 |
EP2734505A1 (de) | 2014-05-28 |
UY34200A (es) | 2013-02-28 |
US20130150325A1 (en) | 2013-06-13 |
WO2013011033A1 (de) | 2013-01-24 |
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