AR040726A1 - Compuesto de 2- fenilpiridin-4-il-heterociclico, composicion farmaceutica que lo comprende y su uso para la fabricacion de un medicamento - Google Patents
Compuesto de 2- fenilpiridin-4-il-heterociclico, composicion farmaceutica que lo comprende y su uso para la fabricacion de un medicamentoInfo
- Publication number
- AR040726A1 AR040726A1 AR20030102722A ARP030102722A AR040726A1 AR 040726 A1 AR040726 A1 AR 040726A1 AR 20030102722 A AR20030102722 A AR 20030102722A AR P030102722 A ARP030102722 A AR P030102722A AR 040726 A1 AR040726 A1 AR 040726A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- halo
- perfluoro
- cyano
- alkoxy
- Prior art date
Links
- 238000004519 manufacturing process Methods 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 239000002131 composite material Substances 0.000 title 1
- 229940126601 medicinal product Drugs 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 15
- 125000005843 halogen group Chemical group 0.000 abstract 8
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 6
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 3
- WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical compound C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 abstract 3
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 abstract 3
- FZWLAAWBMGSTSO-UHFFFAOYSA-N Thiazole Chemical compound C1=CSC=N1 FZWLAAWBMGSTSO-UHFFFAOYSA-N 0.000 abstract 3
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 abstract 3
- 229920006395 saturated elastomer Polymers 0.000 abstract 3
- YLQBMQCUIZJEEH-UHFFFAOYSA-N Furan Chemical compound C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 abstract 2
- SIKJAQJRHWYJAI-UHFFFAOYSA-N Indole Chemical compound C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 abstract 2
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical compound C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 abstract 2
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 abstract 2
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 abstract 2
- KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical compound C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 abstract 2
- SMWDFEZZVXVKRB-UHFFFAOYSA-N Quinoline Chemical compound N1=CC=CC2=CC=CC=C21 SMWDFEZZVXVKRB-UHFFFAOYSA-N 0.000 abstract 2
- YTPLMLYBLZKORZ-UHFFFAOYSA-N Thiophene Chemical compound C=1C=CSC=1 YTPLMLYBLZKORZ-UHFFFAOYSA-N 0.000 abstract 2
- 102000009618 Transforming Growth Factors Human genes 0.000 abstract 2
- 108010009583 Transforming Growth Factors Proteins 0.000 abstract 2
- 239000003814 drug Substances 0.000 abstract 2
- 125000005842 heteroatom Chemical group 0.000 abstract 2
- AWJUIBRHMBBTKR-UHFFFAOYSA-N isoquinoline Chemical compound C1=NC=CC2=CC=CC=C21 AWJUIBRHMBBTKR-UHFFFAOYSA-N 0.000 abstract 2
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 1
- WNXJIVFYUVYPPR-UHFFFAOYSA-N 1,3-dioxolane Chemical compound C1COCO1 WNXJIVFYUVYPPR-UHFFFAOYSA-N 0.000 abstract 1
- BAXOFTOLAUCFNW-UHFFFAOYSA-N 1H-indazole Chemical compound C1=CC=C2C=NNC2=C1 BAXOFTOLAUCFNW-UHFFFAOYSA-N 0.000 abstract 1
- IMSODMZESSGVBE-UHFFFAOYSA-N 2-Oxazoline Chemical compound C1CN=CO1 IMSODMZESSGVBE-UHFFFAOYSA-N 0.000 abstract 1
- VHMICKWLTGFITH-UHFFFAOYSA-N 2H-isoindole Chemical compound C1=CC=CC2=CNC=C21 VHMICKWLTGFITH-UHFFFAOYSA-N 0.000 abstract 1
- MGADZUXDNSDTHW-UHFFFAOYSA-N 2H-pyran Chemical compound C1OC=CC=C1 MGADZUXDNSDTHW-UHFFFAOYSA-N 0.000 abstract 1
- GAMYYCRTACQSBR-UHFFFAOYSA-N 4-azabenzimidazole Chemical compound C1=CC=C2NC=NC2=N1 GAMYYCRTACQSBR-UHFFFAOYSA-N 0.000 abstract 1
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 abstract 1
- 102000018918 Activin Receptors Human genes 0.000 abstract 1
- 108010052946 Activin Receptors Proteins 0.000 abstract 1
- 229910003827 NRaRb Inorganic materials 0.000 abstract 1
- ZCQWOFVYLHDMMC-UHFFFAOYSA-N Oxazole Chemical compound C1=COC=N1 ZCQWOFVYLHDMMC-UHFFFAOYSA-N 0.000 abstract 1
- WYNCHZVNFNFDNH-UHFFFAOYSA-N Oxazolidine Chemical compound C1COCN1 WYNCHZVNFNFDNH-UHFFFAOYSA-N 0.000 abstract 1
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- RFRXIWQYSOIBDI-UHFFFAOYSA-N benzarone Chemical compound CCC=1OC2=CC=CC=C2C=1C(=O)C1=CC=C(O)C=C1 RFRXIWQYSOIBDI-UHFFFAOYSA-N 0.000 abstract 1
- 125000001246 bromo group Chemical group Br* 0.000 abstract 1
- 125000001309 chloro group Chemical group Cl* 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 239000003085 diluting agent Substances 0.000 abstract 1
- 239000003937 drug carrier Substances 0.000 abstract 1
- 125000001153 fluoro group Chemical group F* 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- PZOUSPYUWWUPPK-UHFFFAOYSA-N indole Natural products CC1=CC=CC2=C1C=CN2 PZOUSPYUWWUPPK-UHFFFAOYSA-N 0.000 abstract 1
- RKJUIXBNRJVNHR-UHFFFAOYSA-N indolenine Natural products C1=CC=C2CC=NC2=C1 RKJUIXBNRJVNHR-UHFFFAOYSA-N 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- ZLTPDFXIESTBQG-UHFFFAOYSA-N isothiazole Chemical compound C=1C=NSC=1 ZLTPDFXIESTBQG-UHFFFAOYSA-N 0.000 abstract 1
- CTAPFRYPJLPFDF-UHFFFAOYSA-N isoxazole Chemical compound C=1C=NOC=1 CTAPFRYPJLPFDF-UHFFFAOYSA-N 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 230000001575 pathological effect Effects 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 230000026731 phosphorylation Effects 0.000 abstract 1
- 238000006366 phosphorylation reaction Methods 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 125000003226 pyrazolyl group Chemical group 0.000 abstract 1
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 abstract 1
- JWVCLYRUEFBMGU-UHFFFAOYSA-N quinazoline Chemical compound N1=CN=CC2=CC=CC=C21 JWVCLYRUEFBMGU-UHFFFAOYSA-N 0.000 abstract 1
- 102000005962 receptors Human genes 0.000 abstract 1
- 108020003175 receptors Proteins 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 230000019491 signal transduction Effects 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- VLLMWSRANPNYQX-UHFFFAOYSA-N thiadiazole Chemical compound C1=CSN=N1.C1=CSN=N1 VLLMWSRANPNYQX-UHFFFAOYSA-N 0.000 abstract 1
- 229930192474 thiophene Natural products 0.000 abstract 1
- 150000003852 triazoles Chemical class 0.000 abstract 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 1
Classifications
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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
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- 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
- A61P1/16—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
- A61P13/12—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
- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- 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
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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- 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
- A61P25/28—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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
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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]
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- 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
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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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
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- 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
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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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
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- 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
- C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
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- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Biomedical Technology (AREA)
- Diabetes (AREA)
- Cardiology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Urology & Nephrology (AREA)
- Heart & Thoracic Surgery (AREA)
- Endocrinology (AREA)
- Hospice & Palliative Care (AREA)
- Ophthalmology & Optometry (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Dermatology (AREA)
- Immunology (AREA)
- Emergency Medicine (AREA)
- Vascular Medicine (AREA)
- Reproductive Health (AREA)
- Pulmonology (AREA)
- Gastroenterology & Hepatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Un compuesto de 2-fenilpiridin-4-il-heterociclilo de la fórmula (1), o una de sus sales, solvatos o derivados farmacéuticamente aceptables en el que A es furano, dioxolano, tiofeno, pirrol, imidazol, pirrolidina, pirano, piridina, pirimidina, morfolina, piperidina, oxazol, isoxazol, oxazolina, oxazolidina, tiazol, isotiazol, tiadiazol, benzofurano, indol, isoindol, indazol, imidazopiridina, quinazolina, quinolina, isoquinolina, pirazol o triazol; X es N o CH; R1 es H, alquilo C1-6, alquenilo C1-6, alcoxi C1-6, halo, ciano, perfluoro-alquilo C1-6, perfluoro-alcoxi C1-6, NR5R6, -(CH2)nNR5R6, -O(CH2)nOR7, -O(CH2)n-Het, -O(CH2)nNR5R6, -CONR5R6, -CO(CH2)nNR5R6, -SO2R7, -SO2NR5R6, NR5SO2R7, -NR5COR7, -O(CH2)nCONR5R6; -NR5CO(CH2)nNR5R6 o -C(O)R7; R2 es H, alquilo C1-6, halo, ciano, o perfluoro-alquilo C1-6; R3 es H, o halo; R4 es H, halo, fenilo, alquilo C1-6 o NR5R6, donde R5 y R6 se seleccionan independientemente entre H, Het, cicloalquilo C3-6 opcionalmente sustituido con alquilo C1-6 o con alquilo C1-6 opcionalmente sustituido con Het, alcoxi, ciano o NRaRb (done Ra y Rb que pueden ser iguales o diferentes son H, o alquilo C1-6, o Ra y Rb junto con el átomo de N al que estan unidos pueden formar un anillo saturado de 4, 5, o 6 miembros), o R5 y R6 junto con el átomo de N al que están unidos forman un anillo saturado o insaturado de 3, 4, 5, 6 o 7 miembros que puede contener 1 o más heteroátomos seleccionado entre N, S, o O, y en el que el anillo puede estar adicionalmente sustituido con uno o más sustituyentes seleccionados entre halo (tal como fluoro, cloro, bromo), ciano, CF3, hidroxi, -OCF3, alquilo C1-6 y alcoxi C1-6; R7 se selecciona entre H y alquilo C1-6; Het es un grupo heterociclilo de 6 o 6 miembros, unido por C, que puede ser saturado, insaturado o aromático, que puede contener 1 o más heteroátomos seleccionados entre N, S, o O y que puede estar sustituido con alquilo C1-6; y n es 1-4; con las condiciones de que a) cuando A es tiazol(donde el S del tiazol está en el mismo lado que el resto 4-piridilo); X es N; R1 es H, alquilo C1-6, alcoxi C1-6, halo, ciano, perfluoro-alquilo C1-6 o perfluoro-alcoxi C1-6; R2 es H, alquilo C1-6, halo, ciano o perfluoro-alquilo C1-6; y R3 es H o halo; entonces R4 no es NH2; y b) cuando X es N, A es pirazol (donde el anillo que contiene X está unido al anillo de pirazol en el átomo de C próximo a un N el anillo de pirazol) y R2 es H, entonces R3 no es H. Composición farmacéutica que comprende el compuesto definido precedentemente y un vehículo o diluyente farmacéuticamente aceptable, y uso del mismo para la fabricación de un medicamento. Los derivados de 2-fenilpiridin-4-il-heterociclilo anteriores son inhibidores del factor de crecimiento transformante, de la ruta de senalización de ("TGF")-beta, en particular, de la fosforilación de smad2 o smad3 por el receptor TGF-beta tipo I o receptor de activina tipo quinasa ("ALK")-5, cuya utilidad en medicina se refiere específicamente al tratamiento y prevención de un estado patológico mediado por esta ruta.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GB0217751A GB0217751D0 (en) | 2002-07-31 | 2002-07-31 | Compounds |
GB0314698A GB0314698D0 (en) | 2003-06-24 | 2003-06-24 | Compounds |
Publications (1)
Publication Number | Publication Date |
---|---|
AR040726A1 true AR040726A1 (es) | 2005-04-20 |
Family
ID=31497253
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
AR20030102722A AR040726A1 (es) | 2002-07-31 | 2003-07-29 | Compuesto de 2- fenilpiridin-4-il-heterociclico, composicion farmaceutica que lo comprende y su uso para la fabricacion de un medicamento |
Country Status (7)
Country | Link |
---|---|
US (1) | US20050245520A1 (es) |
EP (1) | EP1539748A1 (es) |
JP (1) | JP2005539000A (es) |
AR (1) | AR040726A1 (es) |
AU (1) | AU2003260345A1 (es) |
TW (1) | TW200417547A (es) |
WO (1) | WO2004013135A1 (es) |
Families Citing this family (56)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB0217783D0 (en) * | 2002-07-31 | 2002-09-11 | Glaxo Group Ltd | Compounds |
UA80296C2 (en) * | 2002-09-06 | 2007-09-10 | Biogen Inc | Imidazolopyridines and methods of making and using the same |
OA12925A (en) | 2002-09-18 | 2006-10-13 | Pfizer Prod Inc | Novel isothiazole and isoxazole compounds as transforming growth factor (TGF) inhibitors. |
EP1542685A1 (en) | 2002-09-18 | 2005-06-22 | Pfizer Products Inc. | Triazole derivatives as transforming growth factor (tgf) inhibitors |
DE60330362D1 (de) | 2002-09-18 | 2010-01-14 | Pfizer Prod Inc | Neue pyrazol-verbindungen als hemmer des transformierenden wachstumsfaktors (tgf) |
PL375980A1 (en) | 2002-09-18 | 2005-12-12 | Pfizer Products Inc. | Novel imidazole compounds as transforming growth factor (tgf) inhibitors |
AP2005003261A0 (en) | 2002-09-18 | 2005-03-31 | Pfizer Prod Inc | Novel oxazole and thiazole compounds as transforming growth factor (TGF) inhibitors. |
CL2004000234A1 (es) * | 2003-02-12 | 2005-04-15 | Biogen Idec Inc | Compuestos derivados 3-(piridin-2-il)-4-heteroaril-pirazol sustituidos, antagonistas de aik5 y/o aik4; composicion farmaceutica y uso del compuesto en el tratamiento de desordenes fibroticos como esclerodermia, lupus nefritico, cicatrizacion de herid |
PA8595001A1 (es) * | 2003-03-04 | 2004-09-28 | Pfizer Prod Inc | Nuevos compuestos heteroaromaticos condensados que son inhibidores del factor de crecimiento transforante (tgf) |
WO2005085241A1 (ja) * | 2004-03-05 | 2005-09-15 | Taisho Pharmaceutical Co., Ltd. | チアゾール誘導体 |
US7781478B2 (en) | 2004-07-14 | 2010-08-24 | Ptc Therapeutics, Inc. | Methods for treating hepatitis C |
TW200639163A (en) * | 2005-02-04 | 2006-11-16 | Genentech Inc | RAF inhibitor compounds and methods |
CA2613522A1 (en) | 2005-06-27 | 2007-01-04 | Exelixis, Inc. | Imidazole based lxr modulators |
CA2620223A1 (en) * | 2005-09-02 | 2007-03-08 | Abbott Laboratories | Novel imidazo based heterocycles |
US20100056505A1 (en) * | 2005-11-21 | 2010-03-04 | Biogen Idec Ma Inc. | Substituted Pyrazalones |
EP2044056B1 (en) * | 2006-07-14 | 2012-08-22 | Novartis AG | Pyrimidine derivatives as alk-5 inhibitors |
EP2121669A2 (en) * | 2007-01-30 | 2009-11-25 | Biogen Idec MA, Inc. | Furanone compounds and methods of making and using the same |
EA201000615A1 (ru) * | 2007-10-17 | 2010-12-30 | Новартис Аг | Производные имидазо[1,2-а]пиридина, применимые в качестве ингибиторов апк (активиноподобной киназы) |
US8343966B2 (en) * | 2008-01-11 | 2013-01-01 | Novartis Ag | Organic compounds |
ES2442930T3 (es) * | 2008-01-11 | 2014-02-14 | Novartis Ag | Pirimidinas como inhibidores de cinasas |
US20120220581A1 (en) | 2009-10-30 | 2012-08-30 | Janssen-Cilag, S.A. | IMIDAZO[1,2-b]PYRIDAZINE DERIVATIVES AND THEIR USE AS PDE10 INHIBITORS |
KR101692126B1 (ko) | 2009-12-18 | 2017-01-02 | 미쓰비시 타나베 파마 코퍼레이션 | 신규 항혈소판약 |
AR080754A1 (es) | 2010-03-09 | 2012-05-09 | Janssen Pharmaceutica Nv | Derivados de imidazo (1,2-a) pirazina y su uso como inhibidores de pde10 |
AR081810A1 (es) | 2010-04-07 | 2012-10-24 | Bayer Cropscience Ag | Piridinilpirazoles biciclicos |
MX2012015252A (es) | 2010-06-30 | 2013-05-30 | Ironwood Pharmaceuticals Inc | Estimuladores de sgc. |
EA201300080A1 (ru) * | 2010-07-05 | 2013-06-28 | Мерк Патент Гмбх | Дипиридильные производные, пригодные для лечения заболеваний, индуцированных киназами |
US8871744B2 (en) * | 2010-07-21 | 2014-10-28 | B & G Partyers, LLC | Compounds and methods for selectively targeting tumor-associated mucins |
CN107266433A (zh) | 2010-11-09 | 2017-10-20 | 铁木医药有限公司 | sGC刺激剂 |
CA2838645C (en) | 2011-06-27 | 2020-03-10 | Janssen Pharmaceutica Nv | 1-aryl-4-methyl-[1,2,4]triazolo[4,3-a]quinoxaline derivatives |
CN104066731B (zh) * | 2011-12-27 | 2016-06-15 | 铁木医药有限公司 | 可用作sgc刺激剂的2-苄基、3-(嘧啶-2-基)取代的吡唑类 |
US9669035B2 (en) | 2012-06-26 | 2017-06-06 | Janssen Pharmaceutica Nv | Combinations comprising PDE 2 inhibitors such as 1-aryl-4-methyl-[1,2,4]triazolo-[4,3-A]]quinoxaline compounds and PDE 10 inhibitors for use in the treatment of neurological of metabolic disorders |
ES2607184T3 (es) | 2012-07-09 | 2017-03-29 | Janssen Pharmaceutica, N.V. | Inhibidores de la enzima fosfodiesterasa 10 |
US20150183781A1 (en) * | 2012-08-07 | 2015-07-02 | Um Pharmauji Sdn. Bhd. | 5-(1H-Pyrazol-4-yl)-1H-Pyrrolo[2,3-b]Pyridine Derivatives as Kinase Inhibitors |
ES2908026T3 (es) | 2013-03-14 | 2022-04-27 | Brigham & Womens Hospital Inc | Composiciones y procedimientos para la expansión y el cultivo de células madre epiteliales |
WO2016025629A1 (en) | 2014-08-12 | 2016-02-18 | The Regents Of The University Of California | Molecular composition for enhancing and rejuvenating maintenance and repair of mammalian tissues |
US10568883B2 (en) | 2014-09-03 | 2020-02-25 | Massachusetts Institute Of Technology | Compositions, systems, and methods for generating inner ear hair cells for treatment of hearing loss |
WO2016210292A1 (en) | 2015-06-25 | 2016-12-29 | Children's Medical Center Corporation | Methods and compositions relating to hematopoietic stem cell expansion, enrichment, and maintenance |
CA3010610A1 (en) | 2016-01-08 | 2017-07-13 | The Brigham And Women's Hospital, Inc. | Production of differentiated enteroendocrine cells and insulin producing cells |
US10201540B2 (en) | 2016-03-02 | 2019-02-12 | Frequency Therapeutics, Inc. | Solubilized compositions for controlled proliferation of stem cells / generating inner ear hair cells using GSK3 inhibitors: I |
US10213511B2 (en) | 2016-03-02 | 2019-02-26 | Frequency Therapeutics, Inc. | Thermoreversible compositions for administration of therapeutic agents |
US11260130B2 (en) | 2016-03-02 | 2022-03-01 | Frequency Therapeutics, Inc. | Solubilized compositions for controlled proliferation of stem cells / generating inner ear hair cells using a GSK3 inhibitor: IV |
JP7080179B2 (ja) | 2016-03-15 | 2022-06-03 | ザ チルドレンズ メディカル センター コーポレーション | 造血幹細胞の増大に関する方法および組成物 |
EP3492461A4 (en) | 2016-07-29 | 2020-02-12 | Shanghai Yingli Pharmaceutical Co. Ltd. | NITROGEN HETEROCYCLIC AROMATIC COMPOUND, PREPARATION METHOD THEREOF, PHARMACEUTICAL COMPOSITION THEREOF AND APPLICATION THEREOF |
CA3043383A1 (en) * | 2016-11-14 | 2018-05-17 | Jiangsu Hengrui Medicine Co., Ltd. | 3,4-bipyridyl pyrazole derivative, and preparation method therefor and medical application thereof |
AU2017386417B2 (en) | 2016-12-30 | 2022-07-14 | Frequency Therapeutics, Inc. | 1H-pyrrole-2,5-dione compounds and methods of using them to induce self-renewal of stem/progenitor supporting cells |
CN110066276B (zh) | 2018-01-24 | 2020-09-18 | 上海璎黎药业有限公司 | 芳香杂环化合物、其中间体、制备方法、药物组合物和应用 |
CN110066277B (zh) | 2018-01-24 | 2021-07-23 | 上海璎黎药业有限公司 | 芳香杂环取代烯烃化合物、其制备方法、药物组合物和应用 |
EP3768267A4 (en) | 2018-03-20 | 2022-04-20 | Icahn School of Medicine at Mount Sinai | KINA INHIBITOR COMPOUNDS AND COMPOSITIONS AND METHODS OF USE |
US20210254006A1 (en) | 2018-06-06 | 2021-08-19 | Ideaya Biosciences, Inc. | Methods of culturing and/or expanding stem cells and/or lineage committed progenitor cells using lactam compounds |
AU2018431586A1 (en) * | 2018-07-09 | 2021-01-21 | Synthis Therapeutics, Inc | Antibody-ALK5 inhibitor conjugates and their uses |
EP3837352A1 (en) | 2018-08-17 | 2021-06-23 | Frequency Therapeutics, Inc. | Compositions and methods for generating hair cells by upregulating jag-1 |
US11617745B2 (en) | 2018-08-17 | 2023-04-04 | Frequency Therapeutics, Inc. | Compositions and methods for generating hair cells by downregulating FOXO |
JP2022515652A (ja) | 2018-12-31 | 2022-02-21 | アイカーン スクール オブ メディシン アット マウント サイナイ | キナーゼ阻害剤化合物及び組成物ならびに使用方法 |
WO2020256721A1 (en) * | 2019-06-19 | 2020-12-24 | Synthis, Llc | Antib0dy-alk5 inhibitor conjugates and their uses |
AU2021223336A1 (en) | 2020-02-19 | 2022-10-06 | Nammi Therapeutics, Inc. | Formulated and/or co-formulated liposome compositions containing TGFB antagonist prodrugs useful in the treatment of cancer and methods thereof |
CN115490687B (zh) * | 2022-09-19 | 2023-10-27 | 国家烟草质量监督检验中心 | 3-苯并呋喃基硫咪唑并吡啶衍生物及其制备方法和应用 |
Family Cites Families (8)
Publication number | Priority date | Publication date | Assignee | Title |
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GB9809869D0 (en) * | 1998-05-09 | 1998-07-08 | Medical Res Council | Inhibition of protein kinases |
GB0007405D0 (en) * | 2000-03-27 | 2000-05-17 | Smithkline Beecham Corp | Compounds |
PE20020506A1 (es) * | 2000-08-22 | 2002-07-09 | Glaxo Group Ltd | Derivados de pirazol fusionados como inhibidores de la proteina cinasa |
GB0027987D0 (en) * | 2000-11-16 | 2001-01-03 | Smithkline Beecham Plc | Compounds |
JP2004517068A (ja) * | 2000-11-16 | 2004-06-10 | スミスクライン・ビーチャム・コーポレイション | 化合物 |
GB0102665D0 (en) * | 2001-02-02 | 2001-03-21 | Glaxo Group Ltd | Compounds |
EP1355903B1 (en) * | 2001-02-02 | 2005-03-16 | SmithKline Beecham Corporation | Pyrazole derivatives against tgf overexpression |
GB0217783D0 (en) * | 2002-07-31 | 2002-09-11 | Glaxo Group Ltd | Compounds |
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2003
- 2003-07-29 EP EP03766385A patent/EP1539748A1/en not_active Withdrawn
- 2003-07-29 US US10/522,969 patent/US20050245520A1/en not_active Abandoned
- 2003-07-29 WO PCT/EP2003/008496 patent/WO2004013135A1/en not_active Application Discontinuation
- 2003-07-29 AU AU2003260345A patent/AU2003260345A1/en not_active Abandoned
- 2003-07-29 JP JP2004525405A patent/JP2005539000A/ja active Pending
- 2003-07-29 AR AR20030102722A patent/AR040726A1/es not_active Application Discontinuation
- 2003-07-29 TW TW092120588A patent/TW200417547A/zh unknown
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WO2004013135A1 (en) | 2004-02-12 |
TW200417547A (en) | 2004-09-16 |
AU2003260345A1 (en) | 2004-02-23 |
US20050245520A1 (en) | 2005-11-03 |
JP2005539000A (ja) | 2005-12-22 |
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