AR082109A1 - Derivados de bipiridilo - Google Patents
Derivados de bipiridiloInfo
- Publication number
- AR082109A1 AR082109A1 ARP110102395A ARP110102395A AR082109A1 AR 082109 A1 AR082109 A1 AR 082109A1 AR P110102395 A ARP110102395 A AR P110102395A AR P110102395 A ARP110102395 A AR P110102395A AR 082109 A1 AR082109 A1 AR 082109A1
- Authority
- AR
- Argentina
- Prior art keywords
- cyy
- denotes
- nyy
- atoms
- het3
- Prior art date
Links
- 125000004429 atom Chemical group 0.000 abstract 8
- 125000004432 carbon atom Chemical group C* 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 229920006395 saturated elastomer Polymers 0.000 abstract 3
- 108091000080 Phosphotransferase Proteins 0.000 abstract 2
- 102000020233 phosphotransferase Human genes 0.000 abstract 2
- 125000001424 substituent group Chemical group 0.000 abstract 2
- 125000000169 tricyclic heterocycle group Chemical group 0.000 abstract 2
- ROFVEXUMMXZLPA-UHFFFAOYSA-N Bipyridyl Chemical group N1=CC=CC=C1C1=CC=CC=N1 ROFVEXUMMXZLPA-UHFFFAOYSA-N 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 108091005682 Receptor kinases Proteins 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000002619 bicyclic group Chemical group 0.000 abstract 1
- 230000033228 biological regulation Effects 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 108090000623 proteins and genes Proteins 0.000 abstract 1
- 102000004169 proteins and genes Human genes 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
Classifications
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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
- 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
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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
- A61K31/435—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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4375—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
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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
- A61K31/435—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
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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
- A61K31/435—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
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
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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
- A61K31/435—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
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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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
- A61K31/495—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
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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
- A61K31/495—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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
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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
- A61K31/535—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
- 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
- A61P17/00—Drugs for dermatological disorders
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- 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
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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
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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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
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- 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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
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- 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
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- 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
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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
- A61P9/10—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
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen 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
- C07D213/72—Nitrogen atoms
- C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
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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
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Oncology (AREA)
- Virology (AREA)
- Rheumatology (AREA)
- Neurology (AREA)
- Physical Education & Sports Medicine (AREA)
- Biomedical Technology (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- AIDS & HIV (AREA)
- Transplantation (AREA)
- Pain & Pain Management (AREA)
- Neurosurgery (AREA)
- Urology & Nephrology (AREA)
- Molecular Biology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Ophthalmology & Optometry (AREA)
- Hematology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Communicable Diseases (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyridine Compounds (AREA)
Abstract
La presente se refiere a derivados de bipiridilo de la fórmula (1) y al uso de tales compuestos, en donde la inhibición, regulación y/o modulación de la transducción de señales por proteínas que consumen ATP como quinasas desempeña un papel importante, en particular a inhibidores de las quinasas TGF-b receptoras y al uso de tales compuestos para el tratamiento de enfermedades inducidas por quinasas, en particular para el tratamiento de tumores.Reivindicación 1: Compuestos de la fórmula (1) en donde: W1, W2, W3 denotan de modo independiente entre sí, N o CR3; R1 denota arilo monocíclico que tiene 5, 6, 7, 8, 9 ó 10 átomos de C o un heteroarilo monocíclico que tiene 5, 6, 7, 8, 9, 10, 11, 12, 13 ó 14 átomos de C y 1, 2, 3, 4 ó 5 átomos de N, O y/o S, cada uno de los cuales puede estar sustituido, de modo independiente entre sí, con al menos un sustituyente seleccionado del grupo que consiste en Y, Hal, CN, CF3, OY; R2 denota Ar, Het1, Het2, NY-Het1 o NY-Het2, con preferencia, denota Ar, Het1 o Het2, cada uno de los cuales puede estar sustituido, de modo independiente entre sí, con R4; R3 denota H, NYY o NY-COY; R4 denota Hal, A, -(CYY)n-OY, -(CYY)n-NYY, (CYY)n-Het3, (CYY)n-O-Het3, SY, NO2, CF3, CN, COOY, -CO-NYY, -NY-COA, -NY-SO2A, -SO2-NYY, S(O)mA, -CO-Het3, -O(CYY)n-NYY, -O(CYY)n-Het3, -NH-COOA, -NH-CO-NYY, -NH-COO-(CYY)n-NYY, -NH-COO-(CYY)n-Het3, -NH-CO-NH-(CYY)n-NYY, -NH-CO-NH(CYY)n-Het3,-OCO-NH-(CYY)n-NYY, -OCO-NH-(CYY)n-Het3, CHO, COA, =S, =NY, =O; Y denota H o A; A denota alquilo no ramificado o ramificado que tiene 1, 2, 3, 4, 5, 6, 7, 8, 9 ó 10 átomos de C, en donde 1, 2, 3,4, 5, 6 ó 7 átomos de H pueden estar reemplazados, de modo independiente entre sí, por Hal y/o en donde uno o dos grupos CH2 pueden estar reemplazados, de modo independiente entre sí, con O, S, SO, SO2, un grupo -CY=CY- y/o un grupo -CºC-; Ar denota un carbociclo mono- o bicíclico saturado, insaturado o aromático que tiene 5, 6, 7, 8, 9 ó 10 átomos de C; Het1 denota un heterociclo mono, bi- o tricíclico saturado o insaturado que tiene 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19 ó 20 átomos de C y 1, 2, 3, 4 ó 5 átomos de N, O y/o S; Het2 denota un heteroarilo mono-, bi- o tricíclico que tiene 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19 ó 20 átomos de C y 1, 2, 3, 4 ó 5 átomos de N, O y/o S; Het3 denota un heterociclo mono, bi- o tricíclico saturado o insaturado que tiene 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19 ó 20 átomos de C y 1, 2, 3, 4 ó 5 átomos de N, O y/o S, que puede estar sustituido, de modo independiente entre sí, con al menos un sustituyente seleccionado del grupo de Hal, A, -(CYY)n-OY, -(CYY)n-NYY, SY, NO2, CN, CF3, COOY, -CO-NYY, -NY-COA, -NY-SO2A, -SO2-NYY, S(O)mA, -NH-COOA, -NH-CO-NYY, CHO, COA, =S, =NY, =O; Hal denota F, Cl, Br o I; m denota 0, 1 ó 2; n denota 0, 1, 2, 3 ó 4; y sus sales, solvatos, tautómeros y estereoisómeros fisiológicamente aceptables, incluyendo sus mezclas en todas las proporciones.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP10006927 | 2010-07-05 |
Publications (1)
Publication Number | Publication Date |
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AR082109A1 true AR082109A1 (es) | 2012-11-14 |
Family
ID=44259587
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP110102395A AR082109A1 (es) | 2010-07-05 | 2011-07-05 | Derivados de bipiridilo |
Country Status (15)
Country | Link |
---|---|
US (2) | US8846931B2 (es) |
EP (1) | EP2590946B1 (es) |
JP (1) | JP5886842B2 (es) |
KR (1) | KR20130131293A (es) |
CN (1) | CN102971293A (es) |
AR (1) | AR082109A1 (es) |
AU (1) | AU2011276193B2 (es) |
BR (1) | BR112012033658A2 (es) |
CA (1) | CA2804285C (es) |
EA (1) | EA201300080A1 (es) |
ES (1) | ES2535656T3 (es) |
IL (1) | IL223978A (es) |
MX (1) | MX2012014537A (es) |
SG (1) | SG186871A1 (es) |
WO (1) | WO2012003912A1 (es) |
Families Citing this family (19)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
NZ613219A (en) | 2008-01-04 | 2014-11-28 | Intellikine Llc | Heterocyclic containing entities, compositions and methods |
US8193182B2 (en) | 2008-01-04 | 2012-06-05 | Intellikine, Inc. | Substituted isoquinolin-1(2H)-ones, and methods of use thereof |
UA115767C2 (uk) | 2011-01-10 | 2017-12-26 | Інфініті Фармасьютікалз, Інк. | Способи отримання ізохінолінонів і тверді форми ізохінолінонів |
US8828998B2 (en) | 2012-06-25 | 2014-09-09 | Infinity Pharmaceuticals, Inc. | Treatment of lupus, fibrotic conditions, and inflammatory myopathies and other disorders using PI3 kinase inhibitors |
EA201590693A1 (ru) * | 2012-10-05 | 2015-08-31 | Ригель Фармасьютикалс, Инк. | Ингибиторы gdf-8 |
GB201312800D0 (en) | 2013-07-17 | 2013-08-28 | Heptares Therapeutics Ltd | mGlu5 modulators |
BR112016016289B1 (pt) | 2014-01-14 | 2023-02-07 | Takeda Pharmaceutical Company Limited | Heteroaris e usos dos mesmos |
EP3094326A4 (en) | 2014-01-14 | 2017-07-26 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
WO2015160975A2 (en) | 2014-04-16 | 2015-10-22 | Infinity Pharmaceuticals, Inc. | Combination therapies |
CN104004762B (zh) * | 2014-05-20 | 2016-03-30 | 南京医科大学附属南京儿童医院 | Tgf-r反义序列及其在制备抗气道炎症反应药物中的应用 |
ES2928084T3 (es) * | 2015-02-20 | 2022-11-15 | Rigel Pharmaceuticals Inc | Inhibidores de GDF-8 |
KR20190033526A (ko) | 2016-06-24 | 2019-03-29 | 인피니티 파마슈티칼스, 인코포레이티드 | 병용 요법 |
WO2018167147A1 (en) | 2017-03-15 | 2018-09-20 | F. Hoffmann-La Roche Ag | Azaindoles as inhibitors of hpk1 |
US10342786B2 (en) | 2017-10-05 | 2019-07-09 | Fulcrum Therapeutics, Inc. | P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD |
HRP20221196T1 (hr) | 2017-10-05 | 2022-12-09 | Fulcrum Therapeutics, Inc. | Inhibitori p38 kinaze smanjuju ekspresiju dux4 i nizvodnih gena u cilju liječenja fshd |
MA54133B1 (fr) | 2018-03-08 | 2022-01-31 | Incyte Corp | Composés d'aminopyrazine diol utilisés comme inhibiteurs de pi3k-y |
WO2020010003A1 (en) | 2018-07-02 | 2020-01-09 | Incyte Corporation | AMINOPYRAZINE DERIVATIVES AS PI3K-γ INHIBITORS |
WO2021142086A1 (en) | 2020-01-08 | 2021-07-15 | Synthis Therapeutics, Inc. | Alk5 inhibitor conjugates and uses thereof |
KR20240025070A (ko) * | 2021-03-29 | 2024-02-26 | 아뷰터스 바이오파마 코포레이션 | 치환된 1-아릴-1'-헤테로아릴 화합물, 치환된 1,1'-비헤테로아릴 화합물 및 이를 사용하는 방법 |
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GB9904387D0 (en) | 1999-02-25 | 1999-04-21 | Pharmacia & Upjohn Spa | Antitumour synergistic composition |
AU4972900A (en) | 1999-04-08 | 2000-11-14 | Arch Development Corporation | Use of anti-vegf antibody to enhance radiation in cancer therapy |
AR040726A1 (es) * | 2002-07-31 | 2005-04-20 | Smithkline Beecham Corp | Compuesto de 2- fenilpiridin-4-il-heterociclico, composicion farmaceutica que lo comprende y su uso para la fabricacion de un medicamento |
GB0218876D0 (en) * | 2002-08-13 | 2002-09-25 | Merck Sharp & Dohme | Therapeutic agents |
WO2004084824A2 (en) | 2003-03-24 | 2004-10-07 | Merck & Co., Inc. | Biaryl substituted 6-membered heterocyles as sodium channel blockers |
US20050014753A1 (en) | 2003-04-04 | 2005-01-20 | Irm Llc | Novel compounds and compositions as protein kinase inhibitors |
US7504401B2 (en) | 2003-08-29 | 2009-03-17 | Locus Pharmaceuticals, Inc. | Anti-cancer agents and uses thereof |
CA2594345C (en) | 2004-12-28 | 2013-11-05 | Kinex Pharmaceuticals, Llc | Compositions and methods of treating cell proliferation disorders |
DK1959955T3 (da) | 2005-12-05 | 2011-02-07 | Pfizer Prod Inc | Fremgangsmåde til behandling af abnorm cellevækst |
US20070191371A1 (en) | 2006-02-14 | 2007-08-16 | Kalypsys, Inc. | Heterocyclic modulators of ppar |
US20080280891A1 (en) | 2006-06-27 | 2008-11-13 | Locus Pharmaceuticals, Inc. | Anti-cancer agents and uses thereof |
ES2500165T3 (es) | 2006-06-29 | 2014-09-30 | Kinex Pharmaceuticals, Llc | Composiciones de biarilo y métodos para modular una cascada de quinasas |
EP2041071B1 (en) | 2006-06-29 | 2014-06-18 | Kinex Pharmaceuticals, LLC | Biaryl compositions and methods for modulating a kinase cascade |
WO2008008059A1 (en) | 2006-07-12 | 2008-01-17 | Locus Pharmaceuticals, Inc. | Anti-cancer agents ans uses thereof |
US8217177B2 (en) | 2006-07-14 | 2012-07-10 | Amgen Inc. | Fused heterocyclic derivatives and methods of use |
JP4751856B2 (ja) | 2007-07-03 | 2011-08-17 | 本田技研工業株式会社 | 車体側部構造 |
US20090069288A1 (en) | 2007-07-16 | 2009-03-12 | Breinlinger Eric C | Novel therapeutic compounds |
WO2009024825A1 (en) | 2007-08-21 | 2009-02-26 | Astrazeneca Ab | 2-pyrazinylbenzimidazole derivatives as receptor tyrosine kinase inhibitors |
PT2231642E (pt) * | 2008-01-11 | 2014-03-12 | Novartis Ag | Pirimidinas como inibidores de quinase |
US8343966B2 (en) | 2008-01-11 | 2013-01-01 | Novartis Ag | Organic compounds |
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BR112012033658A2 (pt) | 2016-11-29 |
ES2535656T3 (es) | 2015-05-13 |
WO2012003912A8 (en) | 2012-03-08 |
EP2590946A1 (en) | 2013-05-15 |
CN102971293A (zh) | 2013-03-13 |
JP2013530192A (ja) | 2013-07-25 |
US8846931B2 (en) | 2014-09-30 |
US20140336201A1 (en) | 2014-11-13 |
JP5886842B2 (ja) | 2016-03-16 |
CA2804285C (en) | 2019-05-14 |
EP2590946B1 (en) | 2015-02-18 |
WO2012003912A1 (en) | 2012-01-12 |
MX2012014537A (es) | 2013-02-21 |
AU2011276193B2 (en) | 2015-01-22 |
CA2804285A1 (en) | 2012-01-12 |
AU2011276193A1 (en) | 2013-02-21 |
US20130102608A1 (en) | 2013-04-25 |
EA201300080A1 (ru) | 2013-06-28 |
AU2011276193A8 (en) | 2013-05-02 |
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