AR080875A1 - Inhibidores de la actividad de la proteina tirosina quinasa - Google Patents
Inhibidores de la actividad de la proteina tirosina quinasaInfo
- Publication number
- AR080875A1 AR080875A1 ARP110101195A ARP110101195A AR080875A1 AR 080875 A1 AR080875 A1 AR 080875A1 AR P110101195 A ARP110101195 A AR P110101195A AR P110101195 A ARP110101195 A AR P110101195A AR 080875 A1 AR080875 A1 AR 080875A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- heterocyclyl
- group
- optionally substituted
- cycloalkyl
- Prior art date
Links
- 230000000694 effects Effects 0.000 title abstract 3
- OUYCCCASQSFEME-QMMMGPOBSA-N L-tyrosine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-QMMMGPOBSA-N 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 102000004169 proteins and genes Human genes 0.000 title 1
- 108090000623 proteins and genes Proteins 0.000 title 1
- OUYCCCASQSFEME-UHFFFAOYSA-N tyrosine Natural products OC(=O)C(N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-UHFFFAOYSA-N 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 71
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 64
- 125000000623 heterocyclic group Chemical group 0.000 abstract 11
- 150000001875 compounds Chemical class 0.000 abstract 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 3
- 125000001072 heteroaryl group Chemical group 0.000 abstract 3
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 abstract 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 2
- 102000004022 Protein-Tyrosine Kinases Human genes 0.000 abstract 2
- 108090000412 Protein-Tyrosine Kinases Proteins 0.000 abstract 2
- 125000003342 alkenyl group Chemical group 0.000 abstract 2
- 125000002947 alkylene group Chemical group 0.000 abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 201000010099 disease Diseases 0.000 abstract 2
- 230000005764 inhibitory process Effects 0.000 abstract 2
- 239000000203 mixture Substances 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- 230000011664 signaling Effects 0.000 abstract 2
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 abstract 1
- 102000009465 Growth Factor Receptors Human genes 0.000 abstract 1
- 108010009202 Growth Factor Receptors Proteins 0.000 abstract 1
- 150000001204 N-oxides Chemical class 0.000 abstract 1
- 108091008605 VEGF receptors Proteins 0.000 abstract 1
- 108010073929 Vascular Endothelial Growth Factor A Proteins 0.000 abstract 1
- 102000009484 Vascular Endothelial Growth Factor Receptors Human genes 0.000 abstract 1
- 102000005789 Vascular Endothelial Growth Factors Human genes 0.000 abstract 1
- 108010019530 Vascular Endothelial Growth Factors Proteins 0.000 abstract 1
- 125000002252 acyl group Chemical group 0.000 abstract 1
- 230000004663 cell proliferation Effects 0.000 abstract 1
- 125000004122 cyclic group Chemical group 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 125000001188 haloalkyl group Chemical group 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 150000004677 hydrates Chemical class 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 239000000651 prodrug Substances 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
- 239000012453 solvate Substances 0.000 abstract 1
Classifications
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- 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
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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
- A61K31/4365—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 having sulfur as a ring hetero atom, e.g. ticlopidine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/005—Enzyme inhibitors
-
- 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
-
- 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
- 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
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
-
- 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
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/06—Dipeptides
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Biophysics (AREA)
- Genetics & Genomics (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Ophthalmology & Optometry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Se refiere a compuestos que inhiben la actividad de la proteína tirosina quinasa. En particular, se refiere a compuestos que inhiben la actividad de la proteína tirosina quinasa de los receptores de los factores de crecimiento, lo que da como resultado la inhibicion de la senalizacion del receptor, por ejemplo, la inhibicion de la senalizacion del receptor del VEGF (factor de crecimiento endotelial vascular). La presente también proporciona compuestos, composiciones y métodos para el tratamiento de enfermedades y condiciones de proliferacion de células y enfermedades, condiciones y desordenes oftálmicos. Reivindicacion 1: Un compuesto que tiene la formula (1), que comprende los N-oxidos, hidratos, solvatos, tautomeros, sales farmacéuticamente aceptables, prodrogas y complejos de los mismos, y mezclas racémicas y escalémicas, diastereomeros y enantiomeros de los mismos, donde D es seleccionado del grupo que consta de un sistema de anillo aromático, heteroaromático, cicloalquilo o heterocíclico, alquilo C1-6-heterociclilo-C(O)-, alquilo C1-6-heterociclilo-alquilo C1-6-N(R6)-C(O)-, (R6)(R6)N-C(O)-O-heterociclilo-C(O)-, heterociclilo-C(O)-, PivO-heterociclilo-C(O)-, alquilo C1-6-O-C(O)-heterociclilo-C(O)-, alquilo C1-6-C(O)-N(R6)-heterociclilo-C(O)-, (alquilo C1-6)(Box)N-heterociclilo-C(O)-, HO-heterociclilo-C(O)-, HO-C(O)-heterociclilo-C(O)-, alquilo C1-6-C(O)-O-heterociclilo-C(O), (R6)(R6)N-alquil C1-6-N(R6)-C(O)-heterociclilo-C(O)-, alquilo C1-6-heterociclilo-C(O)-heterociclilo-C(O)- y (R6)(R6)N-heterociclilo-C(O)-, donde cada uno de los grupos aromáticos, heteroaromáticos, cicloalquilo y heterocíclicos está opcionalmente sustituido con 1 o más R38 seleccionados independientemente; M es una mitad heterocíclica, fusionada, opcionalmente sustituida; Z es seleccionado del grupo que consta de -O-, -S(O)0-2- y -NR5-, en donde R5 es seleccionado del grupo que consta de H, alquilo C1-5 opcionalmente sustituido, un acilo C1-5 opcionalmente sustituido y alquilo C1-6-O-C(O), en donde el alquilo C1-6 está opcionalmente sustituido; Ar es un grupo de la formula (2), donde, A4, A5, A6 y A7 son independientemente seleccionados del grupo que consta de N y -CH-, con la salvedad que no más de dos de A4, A5, A6 y A7 pueden ser N, donde Ar está opcionalmente sustituido; y G es un grupo B-L-T, donde B es seleccionado del grupo que consta de un enlace covalente, -N(R13)-, -N(SO2R13)-, -O-, -S(O)0-2 y -C(=O)-; L es seleccionado del grupo que consta de un enlace covalente, -C(=S)N(R13)-, -C(=NR14)N(R13)-, -SO2N(R13)-, -SO2-, -C(=O)N(R13)-, -N(R13)-, -C(=O)alquilo C1-2-N(R13)-, -N(R13)alquilo C1-2-C(=O)-, -C(=O)alquilo C0-1-C(=O)N(R13)-, -alquileno C0-4, -C(=O)alquilo C0-1-C(=O)OR3-, -C(NR14)alquilo C0-1-C(=O)-, -C(=O)-, -C(=O)alquilo C0-1-C(=O)- y un heterociclilo de cuatro a seis miembros, opcionalmente sustituido, que contiene entre uno y tres heteroátomos anulares incluyendo por lo menos un nitrogeno, en donde el alquilo y el alquileno están opcionalmente sustituidos; y T es seleccionado del grupo que consta de -H, -R13, -alquilo C0-4, -alquilo C0-4-Q, -O-alquilo C0-4-Q, -alquilo C0-4-O-Q, -N(R13)alquilo C0-4-Q, -SO2-alquilo C0-4-Q, -C(=O)alquilo C0-4-Q, -alquilo C0-4-N(R13)Q y -C(=O)N(R13)alquilo C0-4-Q, en donde cada alquilo C0-4 está opcionalmente sustituido; donde R38 es seleccionado del grupo que consta de alquinilo C2-6-heterociclilo, H(O)C- y alquilo C1-6-C(O)-O-alquilo C1-6-C(O)-, R37O-alquilo C1-6-C(O)-heterociclilo-alquilo C1-6-, R37O-(CH2)1-6-N(A)-(CH2)1-4-, alquilo C1-6-S(O)2-(CH2)2-N(A)-CH2-, R37O-(CH2)j-[(CH2)iO]x-(CH2)i1-N(A)-(CH2)j1, -R37O-C(O)-alquilo C0-6-heterociclilo-CH2, R37O-(CH2)j-[(CH2)iO]x-(CH2)i1-N(R39)-C(O)-, R37-O-C(O)-alquilo C1-6-heterociclilo-C(O)-, HOOC-alquilo C1-6-N(A)-CH2-, (HOOC)(NR9R10)-alquilo C1-6-N(A)-CH2-, R37O-C(O)-alquilo C1-6-C(O)-, (R9)(R10)N-alquilo C1-6-C(O)-heterociclilo-CH2-, cicloalquilo-N(R39)-C(O)-O-alquilo C1-6-, R37-O-alquilo C1-6-O-alquilo C1-6-C(O)-, (R9)(R10)N-C(O)-alquilo C1-6-heterociclilo-CH2-, (R9)(R10)N-alquilo C1-6-C(O)-O-alquilo C1-6-heterociclilo-CH2-, NC-alquilo C1-6-heterociclilo-CH2-, F3C-alquilo C1-6-heterociclilo-CH2-, alquilo C1-6-C(O)-O-alquilo C1-6-C(O)-(heterociclilo de 5 - 10 miembros)-alquilo C1-6-, (heterociclilo fusionado de 8 a 10 miembros, opcionalmente sustituido)-alquilo C1-6-, heteroarilo-alquilo C1-6-heterociclilo-alquilo C1-6-, R37-alquilo C1-6-O-alquilo C1-6-heterociclilo-alquilo C1-6-, R37O-C(O)-alquilo C1-6-O-heterociclilo-alquilo C1-6-, R37O-C(O)-alquilo C1-6-heterociclilo-alquilo C1-6-, heterociclilo-alquilo C1-6-O-arilo-N(R6)-alquilo C1-6-, (heteroarilo sustituido con uno o más alquilo C1-6)-N(R6)-alquilo C1-6-, (alquilo C1-6)2N-alquilo C1-6-arilo-N(R6)-alquilo C1-6-, (alquilo C1-6)2N-alquilo C1-6-C(O)-arilo-N(R6)-alquilo C1-6-, heterociclilo-alquilo C1-6-O-arilo-N(R6)-alquilo C1-6-, (R6)2N-heterociclilo-alquilo C1-6-, alquilo C1-6-C(O)-N(R6)-heterociclilo-alquilo C1-6-, alquilo C1-6C(O)-O-alquilo C1-6-C(O)-N(R6)-heterociclilo-alquilo C1-6-, R37O-alquilo C1-6-C(O)-N(R6)-heterociclilo-alquilo C1-6-, heteroarilo-alquilo C1-6-C(O)-N(R6)-heterociclilo-alquilo C1-6-, alquilo C1-6-S(O)2-N(R6)-heterociclilo-alquilo C1-6-, alquilo C1-6-O-C(O)-N(R6)-heterociclilo-alquilo C1-6-, alquilo C1-6-N(R6)-C(O)-N(R6)-heterociclilo-alquilo C1-6-, alquilo C1-6-heterociclilo-C(O)-N(R6)-heterociclilo-alquilo C1-6-, R37O-alquilo C1-6-N(R6)-C(O)-N(R6)-heterociclilo-alquilo C1-6-, (heterociclilo opcionalmente sustituido con uno o más alquilo C1-6)-alquilo C1-6-, (alquilo C1-6)2N-alquilo C1-6-, alquilo C1-6-heterociclilo-C(O)-alquilo C1-6-, heterociclilo-C(O)-alquilo C1-6-, alquilo C1-6-O-C(O)-alquilo C1-6-, alquilo C1-6-O-C(O)-alquilo C1-6-heteroarilo-N(R6)-C(O)-alquilo C1-6-, (alquilo C1-6)2N-heterociclilo-C(O)-alquilo C1-6-, heteroarilo-alquilo C1-6-N(R6)-C(O)-alquilo C1-6-, (Boc)(H)N-heterociclilo-C(O)-alquilo C1-6-, alquilo C1-6-O-C(O)-heterociclilo-C(O)-alquilo C1-6-, Boc-heterociclilo-C(O)-alquilo C1-6-, Ac-O-alquilo C1-6-C(O)-heterociclilo-C(O)-alquilo C1-6-, R37O-alquilo C1-6-C(O)-heterociclilo-C(O)-alquilo C1-6-, (Boc)(H)N-alquilo C1-6-C(O)-heterociclilo-C(O)-alquilo C1-6-, NH2-alquilo C1-6-C(O)-heterociclilo-C(O)-alquilo C1-6-, (alquilo C1-6)(H)N-C(O)-heterociclilo-C(O)-alquilo C1-6-, NH2-heterociclilo-C(O)-alquilo C1-6-, R37O-alquilo C1-6-O-alquilo C1-6-heterociclilo-C(O)-, alquilo C1-6-O-C(O)-N(R6)-heterociclilo-C(O)-, (R6)(R6)N-heterociclilo-C(O)-, (R6)(R6)N-heterociclilo-alquilo C1-6-, heterociclilo-O-alquilo C1-6-, alquilo C1-6-N(R6)-C(O)-N(R6)-heterociclilo-C(O)-, (R6)(R6)N-C(O)-heterociclilo-O-alquilo C1-6-, alquenilo C2-6-C(O)-N(R6)-heterociclilo-alquilo C1-6-, R37O-alquilo C1-6-C(O)-heterociclilo-O-alquilo C1-6-, R37O-alquilo C1-6-N(R6)-heterociclilo-alquilo C1-6-, R37O-(CH2)j-[(CH2)iO]x-alquilo C1-6-N(R6)-heterociclilo-alquilo C1-6-, halo-alquilo C1-6-heterociclilo-alquilo C1-6-, halo-alquilo C1-6-N(R6)-heterociclilo-alquilo C1-6-, R37O-C(O)-alquilo C1-6-N(R6)-heterociclilo-alquilo C1-6-, R37-O-C(O)-alquilo C1-6-N(R6)-C(O)-N(R6)heterociclilo-alquilo C1-6-, (alquilo C1-6)(H)N-C(O)-heterociclilo-N[alquilo C1-6-C(O)-OH]-alquilo C1-6-, alquilo C1-6-O-C(O)-heterociclilo-alquilo C1-6-, HO-C(O)-heterociclilo-alquilo C1-6-, alquilo C1-6-heterociclilo-C(O)-heterociclilo-alquilo C1-6-, R37O-alquilo C1-6-N(R6)-C(O)-heterociclilo-alquilo C1-6-, (R6)(R6)N-alquilo C1-6-N(R6)-CO)-heterociclilo-alquilo C1-6, (alquilo C1-6)(alquilo C1-6)N-heterociclilo-alquilo C1-6-, R37O-alquilo C1-6-C(O)-[(alquilo C1-6)(alquilo C1-6)heterociclilo]-alquilo C1-6-, alquenilo C2-6-C(O)-[(alquilo C1-6)(alquilo C1-6)heterociclilo]-alquilo C1-6-, R37-O-alquilo C1-6-[(alquilo C1-6)(alquilo C1-6)heterociclilo]-alquilo C1-6-, alquilo C1-6-O-alquilo C1-6-N(R6)-alquilo C1-6-, alquilo C1-6-O-alquilo C1-6-N[C(O)-NH-alquilo C1-6]-alquilo C1-6-, alquilo C1-6-O-alquilo C1-6-N[C(O)-alquilo C1-6]-alquilo C1-6-, alquilo C1-6-O-alquilo C1-6-[C(O)-alquilo C1-6-OH]-alquilo C1-6-, R37O-C(O)-alquilo C1-6-C(O)-heterociclilo-alquilo C1-6-, R37O-C(O)-alquilo C1-6-heterociclilo-alquilo C1-6-, espiro-heterociclilo-alquilo C1-6-, R37O-alquilo C1-6-C(O)-espiro-heterociclilo-alquilo C1-6-, R37O-alquilo C1-6-C(O)-heterociclilo-alquilo C1-6-, alquilo C1-6-heterociclilo-alquilo C1-6-, alquilo C1-6-C(O)-O-alquilo C1-6-C(O)-heterociclilo-alquilo C1-6-, heterociclilo-alquilo C1-6-C(O)-heterociclilo-alquilo C1-6-, (R6)(R6)N-alquilo C1-6-C(O)-heterociclilo-alquilo C1-6-, heterociclilo-C(O)-heterociclilo-alquilo C1-6-, (R6)(R6)N-alquenilo C2-6-C(O)-heterociclilo-alquilo C1-6-, heterociclilo-alquenilo C2-8-C(O)-heterociclilo-alquilo C1-6-, (R6)(R6)N-alquilo C1-6-N(R6)-alquilo C1-6-C(O)-heterociclilo-alquilo C1-6-heterociclilo-C(O)-, (R6)(R6)N-C(O)-heterociclilo-alquilo C1-6-, R37O-C(O)-alquilo C1-6-N(R6)-C(O)-heterociclilo-alquilo C1-6-, alquenilo C2-6-C(O)-O-alquilo C1-6-N(R6)-C(O)-heterociclilo-alquilo C1-6-, (R6)(R6)N-C(O)-heterociclilo-C(O)-, R37O-alquilo C1-6-N(R6)-C(O)-heterociclilo-alquilo C1-6-, R37O-alquilo C1-6-heterociclilo-alquilo C1-6-(heterociclilo)-, R37O-C(O)-alquilo C1-6-heterociclilo-C(O)-, R37O-alquilo C1-6-heterociclilo-C(O)-, R37O-alquilo C1-6-C(O)-heterociclilo-C(O)-, alquilo C1-6-O-C(O)-N(R6)-alquilo C1-6-C(O)-O-alquilo C1-6-C(O)-heterociclilo-alquilo C1-6-, R37O-(CH2)n[(CH2)iO]x-alquilo C1-6-N(R6)-C(O)-heterociclilo-alquilo C1-6-HO-heterociclilo-alquilo C1-6-; R37O-cicloalquil-C(O)-heterociclil-alquilo C1-6, y R37O-(CH2)n[(CH2)iO]x-alquilo C1-6-C(O)-N(R6)-heterociclilo-alquilo C1-6-; A es seleccionado del grupo que consta de -C(O)-alquilo C1-6-N(R39)-C(O)-alquilo C1-6-N(R9)(R10), -C(O)-N(R39)-alquilo C1-6, -C(=NR37)-alquilo C1-6, -C(O)-(CH2)n-S(O)2-alquilo C1-6, -C(O)-N(R39)-cicloalquilo, -C(O)-N(R9)(R10), (R37O)(R37aO)P(O)O-alquilo C1-6-C(O)-, -C(=NR37)-H y -alquilo C1-6-CF3; cada R6 es independientemente H o alquilo C1-6; R37 es seleccionado de grupo que consta de H, alquilo C1-6 y cicloalquilo C3-10; R37a es seleccionado del grupo que consta de H, alquilo C1-6 y cicloalquilo C3-10; j es un ente
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| ARP110101191A AR080871A1 (es) | 2010-04-16 | 2011-04-08 | Tieno[3,2-b]piridinas sustituidas como inhibidores de la actividad de la proteina tirosina quinasa |
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| RU2495044C2 (ru) * | 2007-08-29 | 2013-10-10 | Метилджен Инк. | Ингибиторы активности протеинтирозинкиназы |
| EP2332536A1 (en) * | 2008-03-05 | 2011-06-15 | MethylGene Inc. | Inhibitors of protein tyrosine kinase activity |
| AR080875A1 (es) * | 2010-04-16 | 2012-05-16 | Methylgene Inc | Inhibidores de la actividad de la proteina tirosina quinasa |
| US20130096135A1 (en) * | 2011-09-30 | 2013-04-18 | Methylgene Inc. | Selected Inhibitors of Protein Tyrosine Kinase Activity |
| WO2013044360A1 (en) * | 2011-09-30 | 2013-04-04 | Methylgene Inc. | Inhibitors of protein tyrosine kinase activity |
| US20130096088A1 (en) * | 2011-09-30 | 2013-04-18 | Methylgene Inc. | Inhibitors of Protein Tyrosine Kinase Activity |
| EP2791108B1 (en) | 2011-12-15 | 2016-07-27 | Pfizer Limited | Sulfonamide derivatives |
| US10544117B2 (en) | 2014-09-10 | 2020-01-28 | Temple University—Of the Commonwealth System of Higher Education | 5-hydroxytryptamine receptor 7 activity modulators and their method of use |
| WO2016183150A1 (en) * | 2015-05-12 | 2016-11-17 | Temple University-Of The Commonwealth System Of Higher Education | Novel sigma-2 receptor binders and their method of use |
| CN108530464B (zh) * | 2017-03-02 | 2020-10-27 | 深圳海王医药科技研究院有限公司 | 一种多靶点激酶抑制剂 |
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| US20050020619A1 (en) * | 2003-07-24 | 2005-01-27 | Patrick Betschmann | Thienopyridine kinase inhibitors |
| MX2007001216A (es) * | 2004-07-30 | 2007-03-23 | Methylgene Inc | Inhibidores de la senalizacion del receptor del factor de crecimiento endotelial vascular y del receptor del factor de crecimiento del hepatocito. |
| AU2006229343A1 (en) * | 2005-03-28 | 2006-10-05 | Kirin Pharma Kabushiki Kaisha | Thienopyridine derivative, or quinoline derivative, or quinazoline derivative, having c-Met autophosphorylation inhibiting potency |
| JO2787B1 (en) * | 2005-04-27 | 2014-03-15 | امجين إنك, | Alternative amide derivatives and methods of use |
| CN101248080B (zh) * | 2005-05-20 | 2012-09-05 | 梅特希尔基因公司 | Vegf受体和hgf受体信号的抑制剂 |
| CA2611370C (en) * | 2005-05-20 | 2014-11-25 | Oscar Mario Saavedra | Inhibitors of vegf receptor and hgf receptor signaling |
| ES2593279T3 (es) * | 2007-08-29 | 2016-12-07 | Methylgene Inc. | Procesos e intermedios para preparar inhibidores de cinasa heterocíclicos condensados |
| RU2495044C2 (ru) * | 2007-08-29 | 2013-10-10 | Метилджен Инк. | Ингибиторы активности протеинтирозинкиназы |
| EP2332536A1 (en) | 2008-03-05 | 2011-06-15 | MethylGene Inc. | Inhibitors of protein tyrosine kinase activity |
| AR080875A1 (es) * | 2010-04-16 | 2012-05-16 | Methylgene Inc | Inhibidores de la actividad de la proteina tirosina quinasa |
| US20130096088A1 (en) * | 2011-09-30 | 2013-04-18 | Methylgene Inc. | Inhibitors of Protein Tyrosine Kinase Activity |
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