AR086357A1 - Derivados de indazol sustituidos activos como inhibidores de quinasas - Google Patents
Derivados de indazol sustituidos activos como inhibidores de quinasasInfo
- Publication number
- AR086357A1 AR086357A1 ARP120101671A ARP120101671A AR086357A1 AR 086357 A1 AR086357 A1 AR 086357A1 AR P120101671 A ARP120101671 A AR P120101671A AR P120101671 A ARP120101671 A AR P120101671A AR 086357 A1 AR086357 A1 AR 086357A1
- Authority
- AR
- Argentina
- Prior art keywords
- branched
- straight
- optionally substituted
- heterocyclyl
- group selected
- Prior art date
Links
- BAXOFTOLAUCFNW-UHFFFAOYSA-N 1H-indazole Chemical class C1=CC=C2C=NNC2=C1 BAXOFTOLAUCFNW-UHFFFAOYSA-N 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 14
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 10
- 125000001072 heteroaryl group Chemical group 0.000 abstract 10
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 9
- 125000003118 aryl group Chemical group 0.000 abstract 9
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 8
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 8
- 239000001257 hydrogen Substances 0.000 abstract 7
- 229910052739 hydrogen Inorganic materials 0.000 abstract 7
- 150000002431 hydrogen Chemical class 0.000 abstract 6
- 150000001875 compounds Chemical class 0.000 abstract 5
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 201000010099 disease Diseases 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 2
- 239000001301 oxygen Substances 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 abstract 2
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 102000001253 Protein Kinase Human genes 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 230000002074 deregulated effect Effects 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 108060006633 protein kinase Proteins 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000003107 substituted aryl 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
- A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—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
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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
- 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
- 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
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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
- C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
- C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/14—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D295/155—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
- C07D295/18—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
- C07D295/182—Radicals derived from carboxylic acids
- C07D295/185—Radicals derived from carboxylic acids from aliphatic carboxylic acids
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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
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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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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- 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
- C07D403/12—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 chain containing hetero atoms as chain links
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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
- C07D403/14—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 three or more hetero rings
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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
- C07D405/02—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 two hetero rings
- C07D405/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
- C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
- C12N9/10—Transferases (2.)
- C12N9/12—Transferases (2.) transferring phosphorus containing groups, e.g. kinases (2.7)
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- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12Y—ENZYMES
- C12Y207/00—Transferases transferring phosphorus-containing groups (2.7)
- C12Y207/10—Protein-tyrosine kinases (2.7.10)
- C12Y207/10001—Receptor protein-tyrosine kinase (2.7.10.1)
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)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Wood Science & Technology (AREA)
- Zoology (AREA)
- Genetics & Genomics (AREA)
- Biochemistry (AREA)
- General Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Molecular Biology (AREA)
- Biotechnology (AREA)
- Microbiology (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Enzymes And Modification Thereof (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Útiles para tratar enfermedades causadas por una actividad de proteína quinasa desregulada, tal como el cáncer. También proporciona métodos para preparar estos compuestos, composiciones farmacéuticas que comprenden estos compuestos, y métodos para tratar enfermedades utilizando estos compuestos o las composiciones farmacéuticas que los contienen.Reivindicación 1: Un compuesto caracterizado porque tiene la fórmula (1), donde: Ar es un grupo seleccionado entre los compuestos de formula (Ar1), (Ar2) ó (Ar3), donde: R1 es A, NR6R7, OR8, SOnR9, COR10, nitro, ciano o un grupo opcionalmente sustituido seleccionado entre cicloalquilo C3-6, heterociclilo y heteroarilo; R2, R3, R4 y R5 son independientemente hidrógeno, halógeno, nitro, ciano, SOnR9, COR10, NR11R12, OR13 o un grupo opcionalmente sustituido seleccionado entre alquilo C1-6 recto o ramificado, alquenilo C2-6 recto o ramificado, alquinilo C2-6 recto o ramificado, cicloalquilo C3-6 y heterociclilo, donde: A es un alquilo C1-6 recto o ramificado sustituido con un grupo seleccionado entre un heterociclilo opcionalmente sustituido, un heteroarilo opcionalmente sustituido, SOnR9, COR10, NR11R12 y OR13; R6 es hidrógeno o un grupo opcionalmente sustituido seleccionado entre alquilo C1-6 recto o ramificado, alquenilo C2-6 recto o ramificado, alquinilo C2-6 recto o ramificado, C3-6 cicloalquilo, heterociclilo, arilo y heteroarilo; R7 es hidrógeno, SOnR9, COR10, un alquilo C1-6 recto o ramificado sustituido o un grupo opcionalmente sustituido seleccionado entre alquenilo C2-6 recto o ramificado, alquinilo C2-6 recto o ramificado, cicloalquilo C3-6, heterociclilo, arilo y heteroarilo o R6 y R7, tomados juntos con el átomo de nitrógeno al cual están unidos, pueden formar un grupo heterociclilo opcionalmente sustituido; R8 es hidrógeno, A, COR10 o un grupo opcionalmente sustituido seleccionado entre alquenilo C2-6 recto o ramificado, alquinilo C2-6 recto o ramificado, cicloalquilo C3-6, heterociclilo, arilo y heteroarilo, donde A es como se definió más arriba; R9 es NR11R12 o un grupo opcionalmente sustituido seleccionado entre alquilo C1-6 recto o ramificado, alquenilo C2-6 recto o ramificado, alquinilo C2-6 recto o ramificado, cicloalquilo C3-6, heterociclilo, arilo y heteroarilo; R10 es hidrógeno, NR11R12, OR13 o un grupo opcionalmente sustituido seleccionado entre alquilo C1-6 recto o ramificado, alquenilo C2-6 recto o ramificado, alquinilo C2-6 recto o ramificado, cicloalquilo, C3-6 heterociclilo, arilo y heteroarilo; R11 y R12 son independientemente hidrógeno, SOnR9, COR10 o un grupo opcionalmente sustituido seleccionado entre C1-6 alquilo recto o ramificado, alquenilo C2-6 recto o ramificado, alquinilo C2-6 recto o ramificado, cicloalquilo C3-6, heterociclilo, arilo y heteroarilo, donde R9 y R10 son como se definió más arriba, o R11 y R12, tomados juntos con el átomo de nitrógeno al cual están unidos, pueden formar un grupo heterociclilo opcionalmente sustituido; R13 es hidrógeno, COR10 o un grupo opcionalmente sustituido seleccionado entre alquilo C1-6 recto o ramificado, alquenilo C2-6 recto o ramificado, alquinilo C2-6 recto o ramificado, cicloalquilo C3-6, heterociclilo, arilo y heteroarilo, donde R10 es como se definió más arriba; n es 0, 1 ó 2; X es un enlace o un grupo opcionalmente sustituido seleccionado entre alquilo C1-6 recto o ramificado, heterociclilo y arilo; Y es un enlace, oxígeno o un grupo opcionalmente sustituido seleccionado entre alquilo C1-6 recto o ramificado, alquenilo C2-6 recto o ramificado, alquinilo C2-6 recto o ramificado, heterociclilo y arilo; Z es un enlace, oxígeno o un alquilo C1-6 recto o ramificado opcionalmente sustituido; Ar’ es un arilo opcionalmente sustituido o un heteroarilo opcionalmente sustituido; o una sal farmacéuticamente aceptable del mismo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11165882 | 2011-05-12 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR086357A1 true AR086357A1 (es) | 2013-12-04 |
Family
ID=46025764
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP120101671A AR086357A1 (es) | 2011-05-12 | 2012-05-11 | Derivados de indazol sustituidos activos como inhibidores de quinasas |
Country Status (24)
| Country | Link |
|---|---|
| US (4) | US9408850B2 (es) |
| EP (1) | EP2707359B1 (es) |
| JP (1) | JP6396210B2 (es) |
| KR (1) | KR101953272B1 (es) |
| CN (1) | CN103534239B (es) |
| AR (1) | AR086357A1 (es) |
| AU (1) | AU2012252468B2 (es) |
| BR (1) | BR112013028733B1 (es) |
| CA (1) | CA2835478C (es) |
| CL (1) | CL2013003227A1 (es) |
| DK (1) | DK2707359T3 (es) |
| EA (1) | EA023579B1 (es) |
| ES (1) | ES2611779T3 (es) |
| HK (1) | HK1193812A1 (es) |
| HU (1) | HUE031166T2 (es) |
| IL (1) | IL229252A (es) |
| MX (1) | MX342509B (es) |
| PL (1) | PL2707359T3 (es) |
| PT (1) | PT2707359T (es) |
| SG (1) | SG194911A1 (es) |
| SI (1) | SI2707359T1 (es) |
| TW (1) | TWI573790B (es) |
| WO (1) | WO2012152763A1 (es) |
| ZA (1) | ZA201309345B (es) |
Families Citing this family (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR077468A1 (es) | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
| ES2611779T3 (es) | 2011-05-12 | 2017-05-10 | Nerviano Medical Sciences S.R.L. | Derivados de indazol sustituidos activos como inhibidores de quinasas |
| CN103739550B (zh) * | 2014-01-02 | 2016-06-01 | 中国药科大学 | 2,3-二甲基-6-脲-2h-吲唑类化合物及其制备方法与应用 |
| LT3322706T (lt) | 2015-07-16 | 2021-03-10 | Array Biopharma, Inc. | Pakeistieji pirazolo[1,5-a]piridino junginiai, kaip ret kinazės inhibitoriai |
| DE102015012050A1 (de) * | 2015-09-15 | 2017-03-16 | Merck Patent Gmbh | Verbindungen als ASIC-Inhibitoren und deren Verwendungen |
| MX2018005087A (es) | 2015-10-26 | 2019-05-16 | Loxo Oncology Inc | Mutaciones puntuales en cáncer resistente a trk y métodos relacionados con las mismas. |
| US10045991B2 (en) | 2016-04-04 | 2018-08-14 | Loxo Oncology, Inc. | Methods of treating pediatric cancers |
| LT3439662T (lt) | 2016-04-04 | 2024-10-10 | Loxo Oncology, Inc. | Skysti (s)-n-(5-((r)-2-(2,5-difluorofenil)-pirolidin-1-il)- pirazolo [1,5-a]pirimidin-3-il)-3-hidroksipirolidin-1-karboksamido preparatai |
| UA125025C2 (uk) | 2016-04-04 | 2021-12-29 | Локсо Онколоджі, Інк. | Способи лікування дитячих ракових захворювань |
| AU2017268371B2 (en) | 2016-05-18 | 2020-11-19 | Array Biopharma Inc. | Preparation of (S)-N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo(1,5-A)pyrimidin-3-y l)-3-hydroxypyrrolidine-1-carboxamide |
| TWI704148B (zh) | 2016-10-10 | 2020-09-11 | 美商亞雷生物製藥股份有限公司 | 作為ｒｅｔ激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物 |
| JOP20190077A1 (ar) | 2016-10-10 | 2019-04-09 | Array Biopharma Inc | مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret |
| JOP20190092A1 (ar) | 2016-10-26 | 2019-04-25 | Array Biopharma Inc | عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها |
| WO2018136663A1 (en) | 2017-01-18 | 2018-07-26 | Array Biopharma, Inc. | Ret inhibitors |
| CN110267960B (zh) | 2017-01-18 | 2022-04-26 | 阿雷生物药品公司 | 作为RET激酶抑制剂的取代的吡唑并[1,5-a]吡嗪化合物 |
| JOP20190213A1 (ar) | 2017-03-16 | 2019-09-16 | Array Biopharma Inc | مركبات حلقية ضخمة كمثبطات لكيناز ros1 |
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| CN1556702A (zh) * | 2001-09-26 | 2004-12-22 | 具有作为激酶抑制剂的活性的氨基吲唑衍生物、它们的制备方法和含有它们的药物组合物 | |
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| US8354399B2 (en) * | 2008-12-18 | 2013-01-15 | Nerviano Medical Sciences S.R.L. | Substituted indazole derivatives active as kinase inhibitors |
| ES2611779T3 (es) | 2011-05-12 | 2017-05-10 | Nerviano Medical Sciences S.R.L. | Derivados de indazol sustituidos activos como inhibidores de quinasas |
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