AR057960A1 - Inhibidores de proteina quinasa biciclicos - Google Patents
Inhibidores de proteina quinasa biciclicosInfo
- Publication number
- AR057960A1 AR057960A1 ARP060105328A ARP060105328A AR057960A1 AR 057960 A1 AR057960 A1 AR 057960A1 AR P060105328 A ARP060105328 A AR P060105328A AR P060105328 A ARP060105328 A AR P060105328A AR 057960 A1 AR057960 A1 AR 057960A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- alkenyl
- alkynyl
- aryl
- cycloalkyl
- Prior art date
Links
- 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
- 125000000217 alkyl group Chemical group 0.000 abstract 40
- 125000000304 alkynyl group Chemical group 0.000 abstract 22
- 125000000392 cycloalkenyl group Chemical group 0.000 abstract 14
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 13
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 abstract 11
- 125000003118 aryl group Chemical group 0.000 abstract 6
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 6
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 6
- 125000005015 aryl alkynyl group Chemical group 0.000 abstract 5
- 125000001424 substituent group Chemical group 0.000 abstract 5
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 abstract 4
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 3
- 125000004414 alkyl thio group Chemical group 0.000 abstract 3
- 125000005018 aryl alkenyl group Chemical group 0.000 abstract 3
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 3
- 201000010099 disease Diseases 0.000 abstract 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 3
- 125000005843 halogen group Chemical group 0.000 abstract 3
- 125000000027 (C1-C10) alkoxy group Chemical group 0.000 abstract 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 2
- 125000003342 alkenyl group Chemical group 0.000 abstract 2
- 125000002877 alkyl aryl group Chemical group 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000004447 heteroarylalkenyl group Chemical group 0.000 abstract 2
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 2
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 abstract 1
- -1 - CF3 Chemical group 0.000 abstract 1
- 206010020751 Hypersensitivity Diseases 0.000 abstract 1
- 206010061218 Inflammation Diseases 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 102000001253 Protein Kinase Human genes 0.000 abstract 1
- 201000004681 Psoriasis Diseases 0.000 abstract 1
- 125000005090 alkenylcarbonyl group Chemical group 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000004448 alkyl carbonyl group Chemical group 0.000 abstract 1
- 125000005087 alkynylcarbonyl group Chemical group 0.000 abstract 1
- 208000026935 allergic disease Diseases 0.000 abstract 1
- 230000007815 allergy Effects 0.000 abstract 1
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 1
- 208000006673 asthma Diseases 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 150000001602 bicycloalkyls Chemical group 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 210000003169 central nervous system Anatomy 0.000 abstract 1
- 125000004473 dialkylaminocarbonyl group Chemical group 0.000 abstract 1
- 125000000262 haloalkenyl group Chemical group 0.000 abstract 1
- 125000001188 haloalkyl group Chemical group 0.000 abstract 1
- 125000000232 haloalkynyl group Chemical group 0.000 abstract 1
- 125000004475 heteroaralkyl group Chemical group 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000004446 heteroarylalkyl group Chemical group 0.000 abstract 1
- 125000005312 heteroarylalkynyl group Chemical group 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 230000003463 hyperproliferative effect Effects 0.000 abstract 1
- 210000000987 immune system Anatomy 0.000 abstract 1
- 230000004054 inflammatory process Effects 0.000 abstract 1
- 125000004043 oxo group Chemical group O=* 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 108060006633 protein kinase Proteins 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229920006395 saturated elastomer Polymers 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Inhiben enzimas proteína quinasa, y son utiles para el tratamiento y la prevencion de enfermedades hiperproliferativas, tales como cáncer, inflamacion, soriasis, alergia/asma, enfermedades y afecciones del sistema inmunitario, y enfermedades y afecciones del sistema nervioso central. Reivindicacion 1: Un compuesto de la formula (1) o una de sus sales aceptables para uso farmacéutico, donde: R1 es -OR4, -NR4R5, -C(=O)R4, -CO2R4, -CONR4R5, -NO2, -CN, -S(O)j1R4, -SO2NR4R5, -NR4C(=O)R5, - NR4C(=O)OR5, -NR4C(=O)NR5R5a, -NR4S(O)j1R5, -C(=S)OR4, -C(=O)SR4, -NR4C(=NR5)NR4aR5a, -NR4C(=NR5)OR4a, -NR4C(=NR5)SR4a, -OC(=O)OR5, -OC(=O)NR4R5, -OC(=O)SR4, -SC(=O)OR4, o -SC(=O)NR4R5; R2 y R3 son, de manera independiente, alquilo C0-10, cicloalquilo C3-10, bicicloalquilo C5-10, arilo, heteroarilo, aralquilo, heteroaralquilo, heterociclilo, heterobicicloalquilo C5-10 espiroalquilo o heteroespiroalquilo, donde cualquiera de estos está opcionalmente sustituido con uno o más sustituyentes independientes G1; X1 y X2 son, de modo independiente, N o -C-E1; X5 es N, -C-E1, o -N-(E1)aa; X3, X4, X6 y X7 son, de manera independiente, -N-(E1)aa o C; donde por lo menos uno de X3, X4, X5, X6 y X7 es -N-(E1)aa; Q1es halo, -CF3, - OCF3, -OR66, -NR66R77(R66a)j11, -C(=O)R66, -CO2R66, -CONR66R77, -NO2, -CN, -S(O)j11R66, -SO2NR66R77, -NR66C(=O)R77, -NR66C(=O)OR77, -NR66C(=O)NR77R66a, -NR66S(O)j11R77, -C(=S)OR66, -C(=O)SR66, -NR66C(=NR77)NR66aR77a, -NR66C(=NR77)OR66a, - NR66C(=NR77)SR66a, -OC(=O)OR66, -OC(=O)NR66R77, -OC(=O)SR66, -SC(=O)OR66, -SC(=O)NR66R77, alquilo C0-10, alquenilo C2-10, alquinilo C2-10, alcoxiC1-10-alquilo C1-10, alcoxiC1-10-alquenilo C2-10, alcoxiC1-10-alquinilo C2-10, alquiltioC1-10-alquilo C1- 10, alquiltioC1-10-alquenilo C2-10, alquiltioC1-10-alquinilo C2-10, cicloalquilo C3-8, cicloalquenilo C3-8, cicloalquiloC3-8-alquilo C1-10, cicloalqueniloC3-8-alquiloC1-10, cicloalquiloC3-8alquenilo C2-10, cicloalqueniloC3-8-alquenilo C2-10, cicloalquiloC3-8-alquinilo C2-10, cicloalquenilo C3-8-alquinilo C2-10, heterociclilo-alquilo C0-10, heterociclilo-alquenilo C2-10, heterociclilo-alquinilo C2-10, arilo-alquiloC0-10, arilo-alquenilo C2-10, arilo-alquinilo C2-10, hetarilo-alquilo C0- 10, hetarilo-alquenilo C2-10, o hetarilo-alquinilo C2-10, donde cualquiera de los cuales está opcionalmente sustituido con uno o más sustituyentes independientes G11; o Q1 es cualquiera de los compuestos 2 a 31, alcoxiC1-10-alquenilo C2-10, alcoxiC1- 10-alquinilo C2-10, alquiltioC1-10-alquilo C1-10, alquiltioC1-10-alquenilo C2-10, alquiltioC1-10-alquinilo C2-10, cicloalquilo C3-8, cicloalquenilo C3-8, cicloalquiloC3-8-alquilo C1-10, cicloalqueniloC3-8-alquiloC1-10, cicloalquiloC3-8alquenilo C2- 10, cicloalqueniloC3-8-alquenilo C2-10, cicloalquiloC3-8-alquinilo C2-10, cicloalquenilo C3-8-alquinilo C2-10, heterociclilo-alquilo C0-10, heterociclilo-alquenilo C2-10, heterociclilo-alquinilo C2-10, arilo-alquiloC0-10, arilo-alquenilo C2-10, arilo-alquinilo C2-10, hetarilo-alquilo C0-10, hetarilo-alquenilo C2-10, o hetarilo-alquinilo C2-10, donde cualquiera de los estos está opcionalmente sustituido con uno o más sustituyentes independientes halo, oxo, -CF3, -OCF3, -OR222, - NR222R333(R222a)j1a, -C(=O)R222, -CO2R222, -C(=O)NR222R333, -NO2, -CN, -S(=O)j1aR222, -SO2NR222R333, -NR222C(=O)R333, -NR222C(=O)OR333, -NR222C(=O)NR333R222a, -NR222S(O)j1aR333, -C(=S)OR222, -C(=O)SR222, -NR222C(=NR333)NR222aR333a, - NR222C(=NR333)OR222a, -NR222C(=NR333)SR222a, -OC(=O)OR222, -OC(=O)NR222R333, -OC(=O)SR222, -SC(=O)OR222, -SC(=O)NR222R333; R4, R4a, R5, R5a, R6, R6a, R7, R7a, R66, R66a, R77, R77a, R222, R222a, R333, y R333a son, de manera independiente, alquilo C0- 10, alquenilo C2-10, alquinilo C2-10, alcoxiC1-10-alquilo C1-10, alcoxiC1-10-alquenilo C2-10, alcoxiC1-10-alquinilo C2-10, alquiltioC1-10-alquilo C1-10, alquiltioC1-10-alquenilo C2-10, alquiltioC1-10-alquinilo C2-10, cicloalquilo C3-8, cicloalquenilo C3-8, cicloalquiloC3-8-alquilo C1-10, cicloalqueniloC3-8-alquiloC1-10, cicloalquiloC3-8alquenilo C2-10, cicloalqueniloC3-8-alquenilo C2-10, cicloalquiloC3-8-alquinilo C2-10, cicloalquenilo C3-8-alquinilo C2-10, heterociclilo-alquilo C0-10, heterociclilo-alquenilo C2-10, heterociclilo-alquinilo C2-10, arilo-alquiloC0-10, arilo-alquenilo C2-10, arilo-alquinilo C2-10, hetarilo-alquilo C0-10, hetarilo-alquenilo C2-10, o hetarilo-alquinilo C2-10, donde cualquiera de los estos está opcionalmente sustituido con uno o más sustituyentes independientes G111; o en el caso de -NR4R5, -NR5R5a, -NR4aR5a, -NR6R7(R6a)j1, -NR6aR7a, -NR7R6a, NR66R77(R66)j11, -NR77R66a, -NR66aR77a, -NR222R333(R222a)j1a, -NR333R222a, -NR222aR333a, - NR77bR87, -NR78R87 o -NR78R88, entonces R4 y R5, o R5 y R5a, o R4a y R5a, o R6 y R7, o R6a y R7a, o R7 y R6a, o R66 y R77, o R77 y R66a, o R66a y R77a, o R222 y R333, o R333 y R222a, o R222a y R333a, o R77b, y R87, o R78 y R87, o R78 y R88, respectivamente, en forma opcional, se toman junto con el átomo de N al cual están unidos, a fin de formar un anillo saturado o insaturado, de 3 a 10 miembros, donde dicho anillo está opcionalmente sustituido con uno o más sustituyentes independientes G1111, y donde dicho anillo comprende, en forma opcional, uno o más heteroátomos diferentes de N, a los cuales R4 y R5, o R5 y R5a, o R4a y R5a, o R6 y R7, o R6a y R7a, o R7 y R6a, o R66 y R77, o R77 y R66a, o R66a y R77a, o R222 y R333, o R333 y R222a, o R222a y R333a, o R77b, y R87, o R78 y R87, o R78 y R88 están unidos, G111 y G1111 son, de manera independiente alquilo C0-10, alquenilo C2-10, alquinilo C2-10, alcoxiC1-10-alquilo C1-10, alcoxiC1-10-alquenilo C2-10, alcoxiC1- 10-alquinilo C2-10, alquiltioC1-10-alquilo C1-10, alquiltioC1-10-alquenilo C2-10, alquiltioC1-10-alquinilo C2-10, cicloalquilo C3-8, cicloalquenilo C3-8, cicloalquiloC3-8-alquilo C1-10, cicloalqueniloC3-8-alquiloC1-10, cicloalquiloC3-8alquenilo C2- 10, cicloalqueniloC3-8-alquenilo C2-10, cicloalquiloC3-8-alquinilo C2-10, cicloalquenilo C3-8-alquinilo C2-10, heterociclilo-alquilo C0-10, heterociclilo-alquenilo C2-10, heterociclilo-alquinilo C2-10, arilo-alquiloC0-10, arilo-alquenilo C2-10, arilo-alquinilo C2-10, hetarilo-alquilo C0-10, hetarilo-alquenilo C2-10, o hetarilo-alquinilo C2-10, donde cualquiera de los estos está opcionalmente sustituido con uno o más sustituyentes independientes halo, -CF3, -OCF3, -OR77b, -NR77bR87, - C(O)R77b, -CO2R77b, -CO2R77b, -CONR77bR87, -NO2, -CN, -S(O)j5a1R77b, -SO2NR77bR87, -NR77bC(=O)R87, -NR77bC(=O)OR87, -NR77bC(=O)NR78R87, -NR77bS(O)j5aR87, -C(=S)OR77b, -C(=O)SR77b, -NR77bC(=NR87)NR78R88, -NR77bC(=NR87)OR78, -NR77bC(=NR87)SR78, - OC(=O)OR77b, -OC(=O)NR77bR87, -OC(=O)SR77b, -SC(=O)OR77b, -P(O)OR77bOR87, o -SC(=O)NR77bR87; R77b, R87 y R88 son, de manera independiente alquilo C0-10, alquenilo C2-10, alquinilo C2-10, alcoxiC1-10-alquilo C1-10, alcoxiC1-10-alquenilo C2-10, alcoxiC1-10-alquinilo C2-10, alquiltioC1-10-alquilo C1-10, alquiltioC1-10-alquenilo C2-10, alquiltioC1-10-alquinilo C2-10, cicloalquilo C3-8, cicloalquenilo C3-8, cicloalquiloC3-8-alquilo C1-10, cicloalqueniloC3-8-alquiloC1-10, cicloalquiloC3- 8alquenilo C2-10, cicloalqueniloC3-8-alquenilo C2-10, cicloalquiloC3-8-alquinilo C2-10, cicloalquenilo C3-8-alquinilo C2-10, heterociclilo-alquilo C0-10, heterociclilo-alquenilo C2-10, heterociclilo-alquinilo C2-10, alquilcarbonilo C1-10, alquenilcarbonilo C2-10, alquinilcarbonilo C2-10, alcoxicarbonilo C1-10, alcoxicarboniloC1-10alquilo C1-10, monoalquilaminocarbonilo C1-6, dialquilaminocarbonilo C1-6, mono(aril)aminocarbonilo, di(aril)aminocarbonilo, o alquiloC1- 10(aril)aminocarbonilo, donde cualquiera de estos está opcionalmente sustituido con uno o más sustituyentes independientes halo, ciano, hidroxi, nitro, alcoxi C1-10, -SO2N(alquilo C0-4)(alquilo C0-4), o -N(alquilo C0-4)(alquilo C0-4); o R77b, R87 y R88 son, de manera independiente, aril-alquiloC0-10, aril-alquenilo C2-10, aril-alquinilo C2-10, hetaril-alquilo C0-10, hetaril-alquenilo C2-10, hetaril-alquinilo C2-10, mono(alquilo C1-6)aminoalquilo C1-6, di(alquilo C1-6)aminoalquilo C1-6, mono(aril)aminoalquilo C1-6, di(aril)aminoalquilo C1-6 o -N(alquilo C1-6)-alquilo C1-6-arilo, donde cualquiera de estos puede estar opcionalmente sustituido con uno o más sustituyentes independientes halo, ciano, nitro, -O(alquilo C0-4), alquilo C1- 10, alquenilo C2-10, alquinilo C2-10, haloalquilo C1-10, haloalquenilo C2-10, haloalquinilo C2-10, -COOH, alcoxicarbonilo C1-4, -CON(alquilo C0-4)(alquilo C0-10), -SO2N(alquilo C0-4)(alquilo C0-4) o -N(alquilo C0-4)(alquilo C0-4), j1, j1a, j11 y j5a representan, de manera independiente, 0, 1 o 2; y aa es 0 o 1.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US74158805P | 2005-12-02 | 2005-12-02 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR057960A1 true AR057960A1 (es) | 2007-12-26 |
Family
ID=37969677
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP060105328A AR057960A1 (es) | 2005-12-02 | 2006-12-01 | Inhibidores de proteina quinasa biciclicos |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US7648987B2 (es) |
| EP (1) | EP1957496B1 (es) |
| AR (1) | AR057960A1 (es) |
| ES (1) | ES2395835T3 (es) |
| TW (1) | TW200730528A (es) |
| WO (1) | WO2007064993A2 (es) |
Families Citing this family (67)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2305682A1 (en) | 2004-04-02 | 2011-04-06 | OSI Pharmaceuticals, Inc. | 6,6-bicyclic ring substituted heterobicyclic protein kinase inhibitors |
| US20100047338A1 (en) | 2008-03-14 | 2010-02-25 | Angela Brodie | Novel C-17-Heteroaryl Steroidal CYP17 Inhibitors/Antiandrogens, In Vitro Biological Activities, Pharmacokinetics and Antitumor Activity |
| RS51843B (sr) * | 2005-11-17 | 2012-02-29 | Osi Pharmaceuticals Llc. | KONDENZOVANI BICIKLIČNI m TOR INHIBITORI |
| US8575164B2 (en) * | 2005-12-19 | 2013-11-05 | OSI Pharmaceuticals, LLC | Combination cancer therapy |
| WO2007087395A2 (en) * | 2006-01-25 | 2007-08-02 | Osi Pharmaceuticals, Inc. | UNSATURATED mTOR INHIBITORS |
| CN101730700A (zh) * | 2007-05-09 | 2010-06-09 | 雅培制药有限公司 | 用作蛋白激酶抑制剂的稠合杂环化合物 |
| US8124759B2 (en) | 2007-05-09 | 2012-02-28 | Abbott Laboratories | Inhibitors of protein kinases |
| WO2008141140A1 (en) * | 2007-05-09 | 2008-11-20 | Abbott Laboratories | Condensed heterocyclic compounds as inhibitors of protein kinases |
| GB2467670B (en) | 2007-10-04 | 2012-08-01 | Intellikine Inc | Chemical entities and therapeutic uses thereof |
| JP2011510018A (ja) * | 2008-01-18 | 2011-03-31 | オーエスアイ・フアーマスーテイカルズ・インコーポレーテツド | 癌治療のためのイミダゾピラジノール誘導体 |
| US8993580B2 (en) | 2008-03-14 | 2015-03-31 | Intellikine Llc | Benzothiazole kinase inhibitors and methods of use |
| EP2252293B1 (en) * | 2008-03-14 | 2018-06-27 | Intellikine, LLC | Kinase inhibitors and methods of use |
| BRPI0910232A2 (pt) * | 2008-03-19 | 2015-09-29 | Osi Pharm Inc | formas de sais inibidores do mtor |
| US8685995B2 (en) | 2008-03-21 | 2014-04-01 | The University Of Chicago | Treatment with opioid antagonists and mTOR inhibitors |
| EP2283020B8 (en) * | 2008-05-19 | 2012-12-12 | OSI Pharmaceuticals, LLC | Substituted imidazopyr-and imidazotri-azines |
| AU2009268611B2 (en) | 2008-07-08 | 2015-04-09 | Intellikine, Llc | Kinase inhibitors and methods of use |
| WO2010050445A1 (ja) * | 2008-10-27 | 2010-05-06 | 武田薬品工業株式会社 | 二環性化合物 |
| US8476431B2 (en) * | 2008-11-03 | 2013-07-02 | Itellikine LLC | Benzoxazole kinase inhibitors and methods of use |
| US20110269779A1 (en) * | 2008-11-18 | 2011-11-03 | Intellikine, Inc. | Methods and compositions for treatment of ophthalmic conditions |
| US20110251189A1 (en) * | 2008-12-10 | 2011-10-13 | Bhaskar Chandra Das | Hypoxia targeted compounds for cancer diagnosis and therapy |
| CA2761389A1 (en) | 2009-02-05 | 2010-08-12 | Tokai Pharmaceuticals, Inc. | Novel prodrugs of steroidal cyp17 inhibitors/antiandrogens |
| EP2421837A1 (en) | 2009-04-20 | 2012-02-29 | OSI Pharmaceuticals, LLC | Preparation of c-pyrazine-methylamines |
| JP2012526138A (ja) * | 2009-05-07 | 2012-10-25 | オーエスアイ・ファーマシューティカルズ，エルエルシー | 副腎皮質癌を治療するためのｏｓｉ−９０６の使用 |
| EP2456869A4 (en) * | 2009-07-23 | 2013-11-27 | Trustees Of The University Of Princeton | MTOR KINASE HEMMER AS ANTIVIRUS AGENT |
| AU2010284254B2 (en) | 2009-08-17 | 2015-09-17 | Intellikine, Llc | Heterocyclic compounds and uses thereof |
| US20120220595A1 (en) | 2009-11-12 | 2012-08-30 | OSI Pharmaceuticals, LLC | Deuterated Tyrosine Kinase Inhibitors |
| KR101661383B1 (ko) * | 2010-02-08 | 2016-09-29 | 머크 샤프 앤 도메 비.브이. | 8-메틸-1-페닐-이미다졸［1,5-ａ］피라진 화합물 |
| WO2011112666A1 (en) | 2010-03-09 | 2011-09-15 | OSI Pharmaceuticals, LLC | Combination anti-cancer therapy |
| US20120028972A1 (en) * | 2010-07-30 | 2012-02-02 | Lilly Wong | Biomarker assays for detecting or measuring inhibition of tor kinase activity |
| CA2828483A1 (en) | 2011-02-23 | 2012-11-01 | Intellikine, Llc | Combination of kinase inhibitors and uses thereof |
| EP2548877A1 (en) | 2011-07-19 | 2013-01-23 | MSD Oss B.V. | 4-(5-Membered fused pyridinyl)benzamides as BTK-inhibitors |
| ES2950569T3 (es) | 2011-07-19 | 2023-10-11 | Merck Sharp & Dohme | (S)-4-(8-amino-3-(1-(but-2-inoil)pirrolidin-2-il)imidazo[1,5-a]pirazin-1-il)-2-metoxi-n-(piridin-2-il)benzamida como inhibidor de la Btk |
| WO2013152342A1 (en) | 2012-04-06 | 2013-10-10 | OSI Pharmaceuticals, LLC | Anti-cancer mtor inhibitor and anti-androgen combination |
| WO2014052669A1 (en) * | 2012-09-26 | 2014-04-03 | The Regents Of The University Of California | Modulation of ire1 |
| TW201441234A (zh) | 2013-01-23 | 2014-11-01 | Merck Sharp & Dohme | Ｂｔｋ抑制劑 |
| WO2014113932A1 (en) * | 2013-01-23 | 2014-07-31 | Merck Sharp & Dohme Corp. | Btk inhibitors |
| WO2014113942A1 (en) | 2013-01-23 | 2014-07-31 | Merck Sharp & Dohme Corp. | Btk inhibitors |
| AU2014236135A1 (en) | 2013-03-14 | 2015-09-10 | Thomas Jefferson University | Androgen receptor down-regulating agents and uses thereof |
| JP6360881B2 (ja) | 2013-03-22 | 2018-07-18 | ミレニアム ファーマシューティカルズ， インコーポレイテッドＭｉｌｌｅｎｎｉｕｍ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ， Ｉｎｃ． | 触媒的ｍｔｏｒｃ１／２阻害薬及びオーロラａキナーゼの選択的阻害薬の組合せ |
| EP3033088A4 (en) | 2013-08-12 | 2017-03-08 | Tokai Pharmaceuticals, Inc. | Biomarkers for treatment of neoplastic disorders using androgen-targeted therapies |
| JP2016540053A (ja) | 2013-12-05 | 2016-12-22 | アセルタ ファーマ ビー．ブイ． | Ｐｉ３ｋ阻害剤とｂｔｋ阻害剤の治療的組み合わせ |
| US9512092B2 (en) | 2013-12-12 | 2016-12-06 | Albert Einstein College Of Medicine, Inc. | Retinoic acid receptor antagonists as chaperone-mediated autophagy modulators and uses thereof |
| EP3082809B1 (en) | 2013-12-20 | 2021-01-20 | Merck Sharp & Dohme Corp. | Btk inhibitors |
| WO2015095102A1 (en) | 2013-12-20 | 2015-06-25 | Merck Sharp & Dohme Corp. | Btk inhibitors |
| CA2935167C (en) | 2014-01-16 | 2022-02-22 | Musc Foundation For Research Development | Targeted nanocarriers for the administration of immunosuppressive agents |
| US10272083B2 (en) | 2014-01-21 | 2019-04-30 | Acerta Pharma B.V. | Methods of treating chronic lymphocytic leukemia and small lymphocytic leukemia using a BTK inhibitor |
| JP6855243B2 (ja) | 2014-01-24 | 2021-04-07 | エイアイ・セラピューティクス・インコーポレーテッド | 癌治療のためのアピリモド（ａｐｉｌｉｍｏｄ）組成物 |
| WO2015181633A2 (en) | 2014-04-11 | 2015-12-03 | Acerta Pharma B.V. | Methods of blocking the cxcr-4/sdf-1 signaling pathway with inhibitors of bruton's tyrosine kinase |
| TW201613644A (en) | 2014-06-17 | 2016-04-16 | Acerta Pharma Bv | Therapeutic combinations of a BTK inhibitor, a PI3K inhibitor, and/or a JAK-2 inhibitor |
| HRP20211813T1 (hr) | 2014-08-11 | 2022-03-04 | Acerta Pharma B.V. | Terapeutske kombinacije inhibitora btk i inhibitora bcl-2 |
| EP3581184B1 (en) | 2014-11-07 | 2021-02-24 | AI Therapeutics, Inc. | Apilimod for use in the treatment of renal cancer |
| WO2016106629A1 (en) | 2014-12-31 | 2016-07-07 | Merck Sharp & Dohme Corp. | Btk inhibitors |
| WO2016106623A1 (en) | 2014-12-31 | 2016-07-07 | Merck Sharp & Dohme Corp. | Benzamide imidazopyrazine btk inhibitors |
| WO2016106628A1 (en) | 2014-12-31 | 2016-07-07 | Merck Sharp & Dohme Corp. | Btk inhibitors |
| WO2016106624A1 (en) | 2014-12-31 | 2016-07-07 | Merck Sharp & Dohme Corp. | Tertiary alcohol imidazopyrazine btk inhibitors |
| WO2016106627A1 (en) * | 2014-12-31 | 2016-07-07 | Merck Sharp & Dohme Corp. | Btk inhibitors |
| WO2016106626A1 (en) | 2014-12-31 | 2016-07-07 | Merck Sharp & Dohme Corp. | Imidazopyrazine analogs with 3-tertiary carbon substitutions as btk inhibitors |
| FR3037959B1 (fr) * | 2015-06-23 | 2017-08-04 | Servier Lab | Nouveaux derives bicycliques, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
| RS60411B1 (sr) | 2015-07-02 | 2020-07-31 | Acerta Pharma Bv | Čvrsti oblici i formulacije (s)-4-(8-amino-3-(1-(but-2-inoil)pirolidin-2-il)imidazo[1,5-a]pirazin-1-il)-n-(piridin-2-il)benzamida |
| MX2018001073A (es) | 2015-08-06 | 2018-06-12 | Chimerix Inc | Nucleosidos de pirrolopirimidina y analogos de los mismos utiles como agentes antivirales. |
| IL297192A (en) | 2016-04-15 | 2022-12-01 | Cancer Research Tech Ltd | Heterocyclic compounds as ret kinase inhibitors |
| DK3442535T3 (da) | 2016-04-15 | 2022-09-05 | Cancer Research Tech Ltd | Heterocykliske stoffer som as ret-kinase-hæmmere |
| GB201705971D0 (en) | 2017-04-13 | 2017-05-31 | Cancer Res Tech Ltd | Inhibitor compounds |
| SG11201912403SA (en) | 2017-06-22 | 2020-01-30 | Celgene Corp | Treatment of hepatocellular carcinoma characterized by hepatitis b virus infection |
| MX2020002322A (es) * | 2017-09-01 | 2020-10-05 | Optikira Llc | Compuestos y composiciones para la inhibicion de ire1. |
| EP3684771B1 (en) | 2017-09-21 | 2024-11-27 | Chimerix, Inc. | Morphic forms of 4-amino-7-(3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-2-methyl-7h-pyrrolo(2,3-d)pyrimidine-5-carboxamide and uses thereof |
| CA3102279A1 (en) | 2018-06-01 | 2019-12-05 | Cornell University | Combination therapy for pi3k-associated disease or disorder |
Family Cites Families (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5217999A (en) * | 1987-12-24 | 1993-06-08 | Yissum Research Development Company Of The Hebrew University Of Jerusalem | Styryl compounds which inhibit EGF receptor protein tyrosine kinase |
| DE69105495T2 (de) * | 1990-04-02 | 1995-04-06 | Pfizer | Benzylphosphonsäure-tyrosinkinaseinhibitoren. |
| US5302606A (en) * | 1990-04-16 | 1994-04-12 | Rhone-Poulenc Rorer Pharmaceuticals Inc. | Styryl-substituted pyridyl compounds which inhibit EGF receptor tyrosine kinase |
| US6645969B1 (en) * | 1991-05-10 | 2003-11-11 | Aventis Pharmaceuticals Inc. | Aryl and heteroaryl quinazoline compounds which inhibit CSF-1R receptor tyrosine kinase |
| DE69222637T2 (de) | 1991-05-10 | 1998-02-26 | Rhone Poulenc Rorer Int | Bis mono- und bicyclische aryl- und heteroarylderivate mit inhibierender wirkung auf die egf und/oder pdgf-rezeptor tyrosinkinase |
| US6194439B1 (en) * | 1991-05-29 | 2001-02-27 | Pfizer Inc. | Tricyclic polyhydroxylic tyrosine kinase inhibitors |
| MX9304801A (es) * | 1992-08-06 | 1997-06-28 | Warner Lambert Co | 2-toindoles (selenoidoles) disulfuros (seleniduros) relacinados, los cuales inhiben a las proteinas tirosina cinasas y los cuales tienen propiedades anti-tumorales. |
| EP0654024A1 (en) | 1992-08-06 | 1995-05-24 | Warner-Lambert Company | 2-thioindoles (selenoindoles) and related disulfides (selenides) which inhibit protein tyrosine kinases and which have antitumor properties |
| GB9226855D0 (en) | 1992-12-23 | 1993-02-17 | Erba Carlo Spa | Vinylene-azaindole derivatives and process for their preparation |
| JPH07133280A (ja) | 1993-11-09 | 1995-05-23 | Takeda Chem Ind Ltd | セフェム化合物、その製造法および抗菌組成物 |
| GB9624482D0 (en) * | 1995-12-18 | 1997-01-15 | Zeneca Phaema S A | Chemical compounds |
| CH690773A5 (de) | 1996-02-01 | 2001-01-15 | Novartis Ag | Pyrrolo(2,3-d)pyrimide und ihre Verwendung. |
| WO1997034876A1 (en) * | 1996-03-15 | 1997-09-25 | Zeneca Limited | Cinnoline derivatives and use as medicine |
| EA001779B1 (ru) | 1996-05-01 | 2001-08-27 | Эли Лилли Энд Компани | Способ лечения заболеваний, связанных с фактором роста сосудистого эндотелия |
| UA54427C2 (uk) | 1996-05-01 | 2003-03-17 | Елі Ліллі Енд Компані | Спосіб лікування очних захворювань, які пов'язані з фактором васкулярного ендотеліального росту |
| US6232299B1 (en) * | 1996-05-01 | 2001-05-15 | Eli Lilly And Company | Use of protein kinase C inhibitors to enhance the clinical efficacy of oncolytic agents and radiation therapy |
| GB9707800D0 (en) | 1996-05-06 | 1997-06-04 | Zeneca Ltd | Chemical compounds |
| AU753555C (en) | 1998-09-18 | 2003-07-03 | Abbott Gmbh & Co. Kg | Pyrrolopyrimidines as protein kinase inhibitors |
| US6713474B2 (en) * | 1998-09-18 | 2004-03-30 | Abbott Gmbh & Co. Kg | Pyrrolopyrimidines as therapeutic agents |
| WO2000035455A1 (en) | 1998-12-15 | 2000-06-22 | Telik, Inc. | Heteroaryl-aryl ureas as igf-1 receptor antagonists |
| DK1183033T3 (da) | 1999-05-21 | 2006-06-06 | Bristol Myers Squibb Co | Pyrrolotriazininhibitorer af kinaser |
| US6982265B1 (en) * | 1999-05-21 | 2006-01-03 | Bristol Myers Squibb Company | Pyrrolotriazine inhibitors of kinases |
| WO2001072751A1 (en) | 2000-03-29 | 2001-10-04 | Knoll Gesellschaft Mit Beschraenkter Haftung | Pyrrolopyrimidines as tyrosine kinase inhibitors |
| AR035885A1 (es) | 2001-05-14 | 2004-07-21 | Novartis Ag | Derivados de 4-amino-5-fenil-7-ciclobutilpirrolo (2,3-d)pirimidina, un proceso para su preparacion, una composicion farmaceutica y el uso de dichos derivados para la preparacion de una composicion farmaceutica |
| SE0102168D0 (sv) * | 2001-06-19 | 2001-06-19 | Karolinska Innovations Ab | New use and new compounds |
| US6939874B2 (en) | 2001-08-22 | 2005-09-06 | Amgen Inc. | Substituted pyrimidinyl derivatives and methods of use |
| US7115617B2 (en) * | 2001-08-22 | 2006-10-03 | Amgen Inc. | Amino-substituted pyrimidinyl derivatives and methods of use |
| GB0122560D0 (en) * | 2001-09-19 | 2001-11-07 | Aventis Pharma Ltd | Chemical compounds |
| EA007983B1 (ru) | 2001-09-19 | 2007-02-27 | Авентис Фарма С.А. | Индолизины в качестве ингибиторов киназных белков |
| SE0104140D0 (sv) * | 2001-12-07 | 2001-12-07 | Astrazeneca Ab | Novel Compounds |
| ES2283744T3 (es) | 2002-02-14 | 2007-11-01 | Dana-Farber Cancer Institute, Inc. | Metodos y composiciones para el tratamiento de condiciones hiperproliferativas. |
| US20050215564A1 (en) * | 2002-02-14 | 2005-09-29 | Stiles Charles D | Methods and compositions for treating hyperproliferative conditions |
| US7186832B2 (en) * | 2003-02-20 | 2007-03-06 | Sugen Inc. | Use of 8-amino-aryl-substituted imidazopyrazines as kinase inhibitors |
| JP2005089352A (ja) | 2003-09-16 | 2005-04-07 | Kissei Pharmaceut Co Ltd | 新規なイミダゾ［１，５−ａ］ピラジン誘導体、それを含有する医薬組成物およびそれらの用途 |
| BRPI0415395A (pt) | 2003-10-15 | 2006-12-12 | Osi Pharm Inc | composto, métodos para inibir a atividade da proteìna quinase e para tratar um paciente que tenha uma condição que seja mediada pela atividade da proteìna quinase, e, composição |
| EP2305682A1 (en) * | 2004-04-02 | 2011-04-06 | OSI Pharmaceuticals, Inc. | 6,6-bicyclic ring substituted heterobicyclic protein kinase inhibitors |
| RS51843B (sr) * | 2005-11-17 | 2012-02-29 | Osi Pharmaceuticals Llc. | KONDENZOVANI BICIKLIČNI m TOR INHIBITORI |
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2006
- 2006-12-01 AR ARP060105328A patent/AR057960A1/es not_active Application Discontinuation
- 2006-12-04 TW TW095145016A patent/TW200730528A/zh unknown
- 2006-12-04 WO PCT/US2006/046226 patent/WO2007064993A2/en not_active Ceased
- 2006-12-04 US US11/633,301 patent/US7648987B2/en not_active Expired - Fee Related
- 2006-12-04 EP EP06844779A patent/EP1957496B1/en active Active
- 2006-12-04 ES ES06844779T patent/ES2395835T3/es active Active
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| WO2007064993A2 (en) | 2007-06-07 |
| WO2007064993A3 (en) | 2007-07-26 |
| US7648987B2 (en) | 2010-01-19 |
| TW200730528A (en) | 2007-08-16 |
| ES2395835T3 (es) | 2013-02-15 |
| EP1957496B1 (en) | 2012-10-24 |
| EP1957496A2 (en) | 2008-08-20 |
| US20070149521A1 (en) | 2007-06-28 |
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