AR071729A1 - Inhibidores de quinasas simil polo (plk) - Google Patents
Inhibidores de quinasas simil polo (plk)Info
- Publication number
- AR071729A1 AR071729A1 ARP080104179A ARP080104179A AR071729A1 AR 071729 A1 AR071729 A1 AR 071729A1 AR P080104179 A ARP080104179 A AR P080104179A AR P080104179 A ARP080104179 A AR P080104179A AR 071729 A1 AR071729 A1 AR 071729A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- cycloalkyl
- heterocycloalkyl
- heterobicycloaryl
- bicycloaryl
- Prior art date
Links
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
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/14—Drugs for dermatological disorders for baldness or alopecia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/16—Emollients or protectives, e.g. against radiation
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- 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
-
- 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
-
- 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
-
- 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
-
- 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
- A61P37/08—Antiallergic 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
-
- 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
- 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
- C07D487/12—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 three hetero rings
- C07D487/14—Ortho-condensed systems
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Dermatology (AREA)
- Biomedical Technology (AREA)
- Physical Education & Sports Medicine (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Rheumatology (AREA)
- Urology & Nephrology (AREA)
- Heart & Thoracic Surgery (AREA)
- Oncology (AREA)
- Pulmonology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Cardiology (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Communicable Diseases (AREA)
- Pain & Pain Management (AREA)
- Transplantation (AREA)
- Vascular Medicine (AREA)
- Hematology (AREA)
- Toxicology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
Abstract
Tambien se proveen composiciones farmaceuticas, kits y art¡culos de fabricacion que comprenden tales compuestos; metodos e intermediarios de utilidad para preparar los compuestos; y metodos de uso de dichos compuestos. Reivindicacion 1: Un compuesto de la formula (1) y sus sales farmaceuticamente aceptables, caracterizado porque W est seleccionado del grupo que consiste en CR8 y N; Y es -(CR9R10)n-; n est seleccionado del grupo que consiste en 1, 2, 3 y 4; L est ausente o es un ligador que provee 1, 2, 3, 4, 5 o 6 separaciones de tomos entre R7 y el nitrogeno al que L est unido, en donde los tomos del ligador que proveen la separacion est n seleccionados del grupo que consiste en carbono, ox¡geno, nitrogeno y azufre; R1 est seleccionado del grupo que consiste en hidrogeno, ciano, tio, hidroxi, carboniloxi, alcoxi, ariloxi, heteroariloxi, carbonilo, oxicarbonilo, amido, amino, alquilamino C1-10, sulfonamido, imino, sulfonilo, sulfinilo, alquilo C1-10, haloalquilo C1-10, hidroxialquilo C1-10, carbonilalquilo C1-3, tiocarbonilalquilo C1-3, sulfonilalquilo C1-3, sulfinilalquilo C1-3, azaalquilo C1-10, iminoalquilo C1-3, cicloalquil C3-12-alquilo C1-5, heterocicloalquil C3-12-alquilo C1-5, arilalquilo C1-10, heteroarilalquilo C1-5, bicicloaril C9-12-alquilo C1-5, heterobicicloaril C8-12-alquilo C1-5, cicloalquilo C3-12, heterocicloalquilo C3-12, bicicloalquilo C9-12, heterobicicloalquilo C3-12, arilo C4-12, heteroarilo C1-10, bicicloarilo C9-12 y heterobicicloarilo C4-12, cada uno sustituido o no sustituido; R2 est seleccionado del grupo que consiste en hidrogeno, carbonilo, oxicarbonilsulfonilo, sulfinilo, alquilo C1-10, haloalquilo C1-10, carbonilalquilo C1-3, tiocarbonilalquilo C1-3, sulfonilalquilo C1-3, sulfinilalquilo C1-3, azaalquilo C1-10, iminoalquilo C1-3, cicloalquil C3-12-alquilo C1-5, heterocicloalquil C3-12-alquilo C1-5, arilalquilo C1-10, heteroarilalquilo C1-5, bicicloaril C9-12-alquilo C1-5, heterobicicloaril C8-12-alquilo C1-5, cicloalquilo C3-12, heterocicloalquilo C3-12, bicicloalquilo C9-12, heterobicicloalquilo C3-12, arilo C4-12, heteroarilo C1-10, bicicloarilo C9-12 y heterobicicloarilo C4-12, cada uno sustituido o no sustituido o R2 y R1 o R14 se toman juntos para formar un anillo sustituido o no sustituido; R3 es hidrogeno o un sustituyente convertible en vivo en hidrogeno; R4 es halo; R5 est seleccionado del grupo que consiste en hidrogeno, halo, nitro, ciano, tio, oxi, hidroxi, carboniloxi, alcoxi C1-10, aril C4-12-oxi, heteroaril C1-10-oxi, carbonilo, oxicarbonilo, amido, amino, alquilamino C1-10, sulfonamido, imino, sulfonilo, sulfinilo, alquilo C1-10, haloalquilo C1-10, hidroxialquilo C1-10, carbonilalquilo C1-10, tiocarbonilalquilo C1-10, sulfonilalquilo C1-10, sulfinilalquilo C1-10, azaalquilo C1-10, iminoalquilo C1-10, cicloalquil C3-12-alquilo C1-5, heterocicloalquil C3-12-alquilo C1-10, arilalquilo C1-10, heteroaril C1-10-alquilo C1-5, bicicloaril C9-12-alquilo C1-5, heterobicicloaril C8-12-alquilo C1-5, cicloalquilo C3-12, heterocicloalquilo C3-12, bicicloalquilo C9-12, heterobicicloalquilo C3-12, arilo C4-12, heteroarilo C1-10, bicicloarilo C9-12 y heterobicicloarilo C4-12, cada uno sustituido o no sustituido; R6 est seleccionado del grupo que consiste en hidrogeno, carbonilo, sulfonilo, sulfinilo, alquilo C1-10, haloalquilo C1-10, carbonilalquilo C1-3, tiocarbonilalquilo C1-3, sulfonilalquilo C1-3, sulfinilalquilo C1-3, azaalquilo C1-10, iminoalquilo C1-3, cicloalquil C3-12-alquilo C1-5, heterocicloalquil C3-12-alquilo C1-5, arilalquilo C1-10, heteroarilalquilo C1-5, bicicloaril C9-12-alquilo C1-5, heterobicicloaril C8-12-alquilo C1-5, cicloalquilo C3-12, heterocicloalquilo C3-12, bicicloalquilo C9-12, heterobicicloalquilo C3-12, arilo C4-12, heteroarilo C1-10, bicicloarilo C9-12 y heterobicicloarilo C4-12, cada uno sustituido o no sustituido; R7 est seleccionado del grupo que consiste en cicloalquilo C3-12, heterocicloalquilo C3-12, bicicloalquilo C9-12, heterobicicloalquilo C3-12, arilo C4-12, heteroarilo C1-10, bicicloarilo C9-12 y heterobicicloarilo C4-12, cada uno sustituido o no sustituido; R8 est seleccionado del grupo que consiste en hidrogeno, halo, nitro, ciano, tio, oxi, hidroxi, carboniloxi, alcoxi, ariloxi, heteroariloxi, carbonilo, oxicarbonilo, amido, amino, alquilamino C1-10, sulfonamido, imino, sulfonilo, sulfinilo, alquilo C1-10, haloalquilo C1-10, hidroxialquilo C1-10, carbonilalquilo C1-3, tiocarbonilalquilo C1-3, sulfonilalquilo C1-3, sulfinilalquilo C1-3, azaalquilo C1-10, iminoalquilo C1-3, cicloalquil C3-12-alquilo C1-5, heterocicloalquil C3-12-alquilo C1-5, arilalquilo C1-10, heteroarilalquilo C1-5, bicicloaril C9-12-alquilo C1-5, heterobicicloaril C8-12-alquilo C1-5, cicloalquilo C3-12, heterocicloalquilo C3-12, bicicloalquilo C9-12, heterobicicloalquilo C3-12, arilo C4-12, heteroarilo C1-10, bicicloarilo C9-12 y heterobicicloarilo C4-12, cada uno sustituido o no sustituido; R9 y R10 est n seleccionados cada uno, de modo independiente, del grupo que consiste en hidrogeno, halo, nitro, ciano, tio, oxi, hidroxi, carboniloxi, alcoxi C1-10, aril C4-2-oxi, heteroaril C1-10-oxi, carbonilo, oxicarbonilo, amido, amino, alquilamino C1-10, sulfonamido, imino, sulfonilo, sulfinilo, alquilo C1-10, haloalquilo C1-10, hidroxialquilo C1-10, carbonilalquilo C1-10, tiocarbonilalquilo C1-10, sulfonilalquilo C1-10, sulfinilalquilo C1-10, azaalquilo C1-10, iminoalquilo C1-10, cicloalquil C3-12-alquilo C1-5, heterocicloalquil C3-12-alquilo C1-10, arilalquilo C1-10, heteroaril C1-10-alquilo C1-5, bicicloaril C9-12-alquilo C1-5, heterobicicloaril C8-12-alquilo C1-5, cicloalquilo C3-12, heterocicloalquilo C3-12, bicicloalquilo C9-12, heterobicicloalquilo C3-12, arilo C4-12, heteroarilo C1-10, bicicloarilo C9-12 y heterobicicloarilo C4-12, cada uno sustituido o no sustituido o R9 y R10 se toman juntos con el carbono al que est n unidos para formar C=O, C=S, C=NR11 o C=CR12R13; R11 est seleccionado del grupo que consiste en hidrogeno, sulfonilo, sulfinilo, alquilo C1-10, haloalquilo C1-10, hidroxialquilo C1-10, carbonilalquilo C1-10, tiocarbonilalquilo C1-10, sulfonilalquilo C1-10, sulfinilalquilo C1-10, azaalquilo C1-10, iminoalquilo C1-10, cicloalquil C3-12-alquilo C1-5, heterocicloalquil C3-12-alquilo C1-10, arilalquilo C1-10, heteroaril C1-10-alquilo C1-5, bicicloaril C9-12-alquilo C1-5, heterobicicloaril C8-12-alquilo C1-5, heteroalquilo C1-10, cicloalquilo C3-12, heterocicloalquilo C3-12, bicicloalquilo C9-12, heterobicicloalquilo C3-12, arilo C4-12, heteroarilo C1-10, bicicloarilo C9-12 y heterobicicloarilo C4-12, cada uno sustituido o no sustituido; R12 y R13 est n seleccionados cada uno, de modo independiente, del grupo que consiste en hidrogeno, halo, nitro, ciano, oxicarbonilo, amido, alquilo C1-10, haloalquilo C1-10, hidroxialquilo C1-10, carbonilalquilo C1-10, tiocarbonilalquilo C1-10, sulfonilalquilo C1-10, sulfinilalquilo C1-10, azaalquilo C1-10, oxaalquilo C1-10, oxoalquilo C1-10, iminoalquilo C1-10, cicloalquil C3-12-alquilo C1-5, heterocicloalquil C3-12-alquilo C1-10, arilalquilo C1-10, heteroaril C1-10-alquilo C1-5, bicicloaril C9-12-alquilo C1-5, heterobicicloaril C8-12-alquilo C1-5, heteroalquilo C1-10, cicloalquilo C3-12, heterocicloalquilo C3-12, bicicloalquilo C9-12, heterobicicloalquilo C3-12, arilo C4-12, heteroarilo C1-10, bicicloarilo C9-12 y heterobicicloarilo C4-12, cada uno sustituido o no sustituido; R14 est seleccionado del grupo que consiste en alquilo C1-10, haloalquilo C1-10, hidroxialquilo C1-10, carbonilalquilo C1-10, tiocarbonilalquilo C1-10, sulfonilalquilo C1-10, sulfinilalquilo C1-10, azaalquilo C1-10, iminoalquilo C1-10, cicloalquil C3-12-alquilo C1-5, heterocicloalquil C3-12-alquilo C1-10, arilalquilo C1-10, heteroaril C1-10-alquilo C1-5, bicicloaril C9-12-alquilo C1-5, heterobicicloaril C8-12-alquilo C1-5, heteroalquilo C1-10, cicloalquilo C3-12, heterocicloalquilo C3-12, bicicloalquilo C9-12, heterobicicloalquilo C3-12, arilo C4-12, heteroarilo C1-10, bicicloarilo C9-12 y heterobicicloarilo C4-12, cada uno sustituido o no sustituido; R32 y R33 se toman juntos para formar X o R32 y R33 est n seleccionados cada uno, de modo independiente, del grupo que consiste en hidrogeno, halo, nitro, ciano, tio, oxi, hidroxi, carboniloxi, alcoxi C1-10, aril C4-12-oxi, heteroaril C1-10-oxi, carbonilo, oxicarbonilo, amido, amino, alquilamino C1-10, sulfonamido, imino, sulfonilo, sulfinilo, alquilo C1-10, haloalquilo C1-10, hidroxialquilo C1-10, carbonilalquilo C1-10, tiocarbonilalquilo C1-10, sulfonilalquilo C1-10, sulfinilalquilo C1-10, azaalquilo C1-10, oxaalquilo C1-10, oxoalquilo C1-10, iminoalquilo C1-10, cicloalquil C3-12-alquilo C1-5, heterocicloalquil C3-12-alquilo C1-10, arilalquilo C1-10, heteroaril C1-10-alquilo C1-5, bicicloaril C9-12-alquilo C1-5, heterobicicloaril C8-12-alquilo C1-5, heteroalquilo C1-10, cicloalquilo C3-12, heterocicloalquilo C3-12, bicicloalquilo C9-12, heterobicicloalquilo C3-12, arilo C4-12, heteroarilo C1-10, bicicloarilo C9-12 y heterobicicloarilo C4-12, cada uno sustituido o no sustituido; y X est seleccionado del grupo que consiste en NR14, O y S, o dos R2, R5, R6, R9, R10 R32 y R33 cualesquiera se toman juntos para formar un anillo sustituido o no sustituido; p est seleccionado del grupo que consiste en 0 y 1; R34 est seleccionado del grupo que consiste en -CONJ34-, -NJ34CO-, -NJ34-, -SO2NJ34-, -NJ34SO2-, J34 est seleccionado del grupo que consiste en hidrogeno y alquilo C1-4; R35 est seleccionado del grupo que consiste en amino, arilo C4-12, heteroarilo C1-10, cicloalquilo C3-8, heterocicloalquilo C3-6, bicicloalquilo C7-12, heterobicicloalquilo C3-12, cada uno sustituido o no sustituido; q est seleccionado del grupo que consiste en 0 y 1; R36 est seleccionado del grupo que consiste en alquilo C1-4, azaalquilo C1-4, cicloalquilo C3-8, heterocicloalquilo C3-8, cada uno sustituido o no sustituido; r est seleccionado del grupo que consiste en 0 y 1; R37 es cicloalquilo C3-8 opcionalmente s
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US97512707P | 2007-09-25 | 2007-09-25 | |
US3730308P | 2008-03-17 | 2008-03-17 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR071729A1 true AR071729A1 (es) | 2010-07-14 |
Family
ID=40219644
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP080104179A AR071729A1 (es) | 2007-09-25 | 2008-09-25 | Inhibidores de quinasas simil polo (plk) |
Country Status (27)
Country | Link |
---|---|
US (4) | US20110201818A1 (es) |
EP (3) | EP2564850B1 (es) |
JP (2) | JP5372939B2 (es) |
KR (2) | KR20140097440A (es) |
CN (2) | CN101917995A (es) |
AR (1) | AR071729A1 (es) |
AU (1) | AU2008304417B2 (es) |
BR (1) | BRPI0817315A2 (es) |
CA (2) | CA2699607A1 (es) |
CL (1) | CL2008002852A1 (es) |
CO (1) | CO6270231A2 (es) |
CR (1) | CR11370A (es) |
DO (1) | DOP2010000091A (es) |
EA (1) | EA019487B1 (es) |
EC (1) | ECSP10010129A (es) |
ES (1) | ES2488966T3 (es) |
GE (1) | GEP20125704B (es) |
HK (1) | HK1145144A1 (es) |
MA (1) | MA31763B1 (es) |
MX (2) | MX2010003249A (es) |
MY (1) | MY152283A (es) |
NZ (1) | NZ584760A (es) |
PE (1) | PE20090710A1 (es) |
TN (1) | TN2010000131A1 (es) |
TW (1) | TWI436769B (es) |
WO (2) | WO2009042711A1 (es) |
ZA (1) | ZA201002543B (es) |
Families Citing this family (25)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP5243970B2 (ja) | 2006-02-14 | 2013-07-24 | バーテックス ファーマシューティカルズ インコーポレイテッド | タンパク質キナーゼの阻害剤として有用なジヒドロジアゼピン |
ES2488966T3 (es) * | 2007-09-25 | 2014-09-01 | Takeda Pharmaceutical Company Limited | Inhibidores de cinasa de tipo Polo |
CN101878216B (zh) * | 2007-09-28 | 2013-07-10 | 西克拉塞尔有限公司 | 作为蛋白激酶抑制剂的嘧啶衍生物 |
JP2011527667A (ja) * | 2008-06-18 | 2011-11-04 | 武田薬品工業株式会社 | ハロ置換ピリミドジアゼピン |
AU2010232644A1 (en) | 2009-03-31 | 2011-10-20 | Arqule, Inc. | Substituted tetrahydropyrazolo-pyrido-azepin compounds |
CA2756568C (en) | 2009-04-06 | 2018-02-13 | University Health Network | Kinase inhibitors and method of treating cancer with same |
SG179207A1 (en) | 2009-09-25 | 2012-04-27 | Vertex Pharma | Methods for preparing pyrimidine derivatives useful as protein kinase inhibitors |
JP2013505927A (ja) | 2009-09-25 | 2013-02-21 | バーテックス ファーマシューティカルズ インコーポレイテッド | プロテインキナーゼ阻害剤として有用なピリミジン誘導体の調製方法 |
WO2011079114A1 (en) | 2009-12-23 | 2011-06-30 | Elan Pharmaceuticals, Inc. | Pteridinones as inhibitors of polo - like kinase |
EP2556070B1 (en) | 2010-04-06 | 2017-06-07 | University Health Network | Synthesis of chiral 2-(1h-indazol-6-yl)-spiro[cyclopropane-1,3'- indolin]-2'-ones |
WO2012061342A2 (en) | 2010-11-01 | 2012-05-10 | Arqule, Inc. | Substituted benzo-imidazo-pyrido-diazepine compounds |
JP5986566B2 (ja) * | 2011-07-07 | 2016-09-06 | イハラケミカル工業株式会社 | ニトロベンゼン化合物の製造方法 |
WO2013058344A1 (ja) * | 2011-10-21 | 2013-04-25 | 武田薬品工業株式会社 | Plk1阻害剤の効果を予測する方法 |
DK3057965T3 (en) * | 2013-10-18 | 2019-04-01 | Univ Health Network | SALT AND CRYSTAL FORMS OF PLK-4 INHIBITOR |
JP2017504653A (ja) | 2014-01-31 | 2017-02-09 | ダナ−ファーバー キャンサー インスティテュート, インコーポレイテッド | ジアミノピリミジンベンゼンスルホン誘導体およびその使用 |
JP2017504651A (ja) | 2014-01-31 | 2017-02-09 | ダナ−ファーバー キャンサー インスティテュート, インコーポレイテッド | ジアゼパン誘導体の使用 |
JP2017526741A (ja) | 2014-08-08 | 2017-09-14 | ダナ−ファーバー キャンサー インスティテュート, インコーポレイテッド | ジアゼパン誘導体およびその使用 |
WO2016201370A1 (en) | 2015-06-12 | 2016-12-15 | Dana-Farber Cancer Institute, Inc. | Combination therapy of transcription inhibitors and kinase inhibitors |
KR20180049058A (ko) | 2015-09-11 | 2018-05-10 | 다나-파버 캔서 인스티튜트 인크. | 시아노 티에노트리아졸로디아제핀 및 그의 용도 |
CN108472299A (zh) | 2015-09-11 | 2018-08-31 | 达纳-法伯癌症研究所股份有限公司 | 乙酰胺噻吩并***并二氮杂环庚三烯及其用途 |
MX2018006499A (es) | 2015-11-25 | 2018-08-01 | Dana Farber Cancer Inst Inc | Inhibidores de bromodominio bivalentes y usos de los mismos. |
TWI763668B (zh) * | 2016-05-05 | 2022-05-11 | 美商嘉來克生命科學有限責任公司 | 整合應激途徑之調節劑 |
KR102337029B1 (ko) * | 2020-03-27 | 2021-12-09 | (주) 업테라 | Plk1 선택적 분해 유도 화합물 |
WO2022145989A1 (ko) * | 2020-12-31 | 2022-07-07 | (주) 업테라 | 선택적 plk1 억제제로서의 피리미도디아제핀 유도체 |
US20240140962A1 (en) * | 2021-02-08 | 2024-05-02 | Medshine Discovery Inc. | 5,6-dihydrothieno[3,4-h]quinazoline compound |
Family Cites Families (25)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US3710795A (en) | 1970-09-29 | 1973-01-16 | Alza Corp | Drug-delivery device with stretched, rate-controlling membrane |
GB1429184A (en) | 1972-04-20 | 1976-03-24 | Allen & Hanburys Ltd | Physically anti-inflammatory steroids for use in aerosols |
US4044126A (en) | 1972-04-20 | 1977-08-23 | Allen & Hanburys Limited | Steroidal aerosol compositions and process for the preparation thereof |
USRE28819E (en) | 1972-12-08 | 1976-05-18 | Syntex (U.S.A.) Inc. | Dialkylated glycol compositions and medicament preparations containing same |
US4410545A (en) | 1981-02-13 | 1983-10-18 | Syntex (U.S.A.) Inc. | Carbonate diester solutions of PGE-type compounds |
US4328245A (en) | 1981-02-13 | 1982-05-04 | Syntex (U.S.A.) Inc. | Carbonate diester solutions of PGE-type compounds |
US4358603A (en) | 1981-04-16 | 1982-11-09 | Syntex (U.S.A.) Inc. | Acetal stabilized prostaglandin compositions |
US4409239A (en) | 1982-01-21 | 1983-10-11 | Syntex (U.S.A.) Inc. | Propylene glycol diester solutions of PGE-type compounds |
US7169778B2 (en) | 1999-09-15 | 2007-01-30 | Warner-Lambert Company | Pteridinones as kinase inhibitors |
ATE380814T1 (de) | 1999-09-17 | 2007-12-15 | Abbott Gmbh & Co Kg | Kinaseinhibitoren als arzneimittel |
KR100955589B1 (ko) | 2001-09-04 | 2010-04-30 | 베링거 잉겔하임 파르마 게엠베하 운트 코 카게 | 신규한 디하이드로프테리디논, 이의 제조방법 및 이를 함유하는 약제학적 조성물 |
US6806272B2 (en) * | 2001-09-04 | 2004-10-19 | Boehringer Ingelheim Pharma Kg | Dihydropteridinones, processes for preparing them and their use as pharmaceutical compositions |
US6861422B2 (en) * | 2003-02-26 | 2005-03-01 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Dihydropteridinones, processes for preparing them and their use as pharmaceutical compositions |
US20060074088A1 (en) | 2004-08-14 | 2006-04-06 | Boehringer Ingelheim International Gmbh | Dihydropteridinones for the treatment of cancer diseases |
EP1630163A1 (de) * | 2004-08-25 | 2006-03-01 | Boehringer Ingelheim Pharma GmbH & Co.KG | Dihydropteridinonderivative, Verfahren zu deren Herstellung und deren Verwendung als Arzneimittel |
EP1632493A1 (de) * | 2004-08-25 | 2006-03-08 | Boehringer Ingelheim Pharma GmbH & Co.KG | Dihydropteridinonderivative, Verfahren zu deren Herstellung und deren Verwendung als Arzneimittel |
CA2578560A1 (en) * | 2004-08-27 | 2006-03-02 | Boehringer Ingelheim International Gmbh | Dihydropteridinones, method for the production thereof, and use thereof as a medicament |
JP5243970B2 (ja) * | 2006-02-14 | 2013-07-24 | バーテックス ファーマシューティカルズ インコーポレイテッド | タンパク質キナーゼの阻害剤として有用なジヒドロジアゼピン |
CN101448830A (zh) | 2006-05-19 | 2009-06-03 | 阿斯利康(瑞典)有限公司 | 作为抗增殖剂的二氢碟啶化合物 |
TW200808325A (en) | 2006-07-06 | 2008-02-16 | Astrazeneca Ab | Novel compounds |
MX2009010034A (es) * | 2007-03-22 | 2009-10-12 | Hoffmann La Roche | Pirimidodiazepinas sustituidas utiles inhibidores de la plk1. |
AU2008287339A1 (en) | 2007-08-15 | 2009-02-19 | Vertex Pharmaceuticals Incorporated | 4-(9-(3, 3-difluorocyclopentyl) -5, 7, 7-trimethyl-6-oxo-6, 7, 8, 9-tetrahydro-5H-pyrimido [4, 5-b][1, 4] diazepin-2-ylamino)-3-methoxybenzamide Derivatives as Inhibitors of the Human Protein Kinases PLK1 to PLK4 for the Treatment of Proliferative Diseases |
ES2488966T3 (es) * | 2007-09-25 | 2014-09-01 | Takeda Pharmaceutical Company Limited | Inhibidores de cinasa de tipo Polo |
CN101878216B (zh) | 2007-09-28 | 2013-07-10 | 西克拉塞尔有限公司 | 作为蛋白激酶抑制剂的嘧啶衍生物 |
JP2011527667A (ja) | 2008-06-18 | 2011-11-04 | 武田薬品工業株式会社 | ハロ置換ピリミドジアゼピン |
-
2008
- 2008-09-24 ES ES08834219.1T patent/ES2488966T3/es active Active
- 2008-09-24 EA EA201070395A patent/EA019487B1/ru not_active IP Right Cessation
- 2008-09-24 CN CN2008801169537A patent/CN101917995A/zh active Pending
- 2008-09-24 MX MX2010003249A patent/MX2010003249A/es active IP Right Grant
- 2008-09-24 CA CA2699607A patent/CA2699607A1/en not_active Abandoned
- 2008-09-24 US US12/680,183 patent/US20110201818A1/en not_active Abandoned
- 2008-09-24 BR BRPI0817315 patent/BRPI0817315A2/pt not_active IP Right Cessation
- 2008-09-24 GE GEAP200811771A patent/GEP20125704B/en unknown
- 2008-09-24 MY MYPI20101261 patent/MY152283A/en unknown
- 2008-09-24 WO PCT/US2008/077558 patent/WO2009042711A1/en active Application Filing
- 2008-09-24 NZ NZ584760A patent/NZ584760A/en not_active IP Right Cessation
- 2008-09-24 KR KR1020147017278A patent/KR20140097440A/ko not_active Application Discontinuation
- 2008-09-24 EP EP12189293.9A patent/EP2564850B1/en active Active
- 2008-09-24 US US12/237,306 patent/US8026234B2/en not_active Expired - Fee Related
- 2008-09-24 EP EP08834219.1A patent/EP2205241B1/en active Active
- 2008-09-24 KR KR1020107009029A patent/KR101444924B1/ko not_active IP Right Cessation
- 2008-09-24 CN CN2012105686507A patent/CN103122001A/zh active Pending
- 2008-09-24 JP JP2010526067A patent/JP5372939B2/ja not_active Expired - Fee Related
- 2008-09-24 AU AU2008304417A patent/AU2008304417B2/en not_active Ceased
- 2008-09-25 TW TW097137049A patent/TWI436769B/zh not_active IP Right Cessation
- 2008-09-25 US US12/680,142 patent/US8202990B2/en not_active Expired - Fee Related
- 2008-09-25 PE PE2008001672A patent/PE20090710A1/es not_active Application Discontinuation
- 2008-09-25 CL CL2008002852A patent/CL2008002852A1/es unknown
- 2008-09-25 EP EP08833760A patent/EP2197442B1/en not_active Not-in-force
- 2008-09-25 WO PCT/US2008/077746 patent/WO2009042806A1/en active Application Filing
- 2008-09-25 AR ARP080104179A patent/AR071729A1/es unknown
- 2008-09-25 CA CA2700295A patent/CA2700295A1/en not_active Abandoned
- 2008-09-25 MX MX2010003244A patent/MX2010003244A/es active IP Right Grant
- 2008-09-25 JP JP2010526073A patent/JP2010540464A/ja active Pending
-
2010
- 2010-03-22 TN TNP2010000131A patent/TN2010000131A1/fr unknown
- 2010-03-25 DO DO2010000091A patent/DOP2010000091A/es unknown
- 2010-04-08 MA MA32753A patent/MA31763B1/fr unknown
- 2010-04-09 CO CO10041197A patent/CO6270231A2/es active IP Right Grant
- 2010-04-12 ZA ZA2010/02543A patent/ZA201002543B/en unknown
- 2010-04-14 CR CR11370A patent/CR11370A/es unknown
- 2010-04-23 EC EC2010010129A patent/ECSP10010129A/es unknown
- 2010-12-07 US US12/962,557 patent/US8318727B2/en not_active Expired - Fee Related
- 2010-12-14 HK HK10111664.0A patent/HK1145144A1/xx not_active IP Right Cessation
Also Published As
Similar Documents
Publication | Publication Date | Title |
---|---|---|
AR071729A1 (es) | Inhibidores de quinasas simil polo (plk) | |
AR071811A1 (es) | Derivados de diazol como activadores de glucoquinasa | |
AR072936A1 (es) | Derivados piridazin y pirimidin condensados con heterociclos nitrogenados, composiciones farmaceuticas que los contienen y uso de los mismos como agentes anticancer. | |
AR071452A1 (es) | Inhibidores de hsp90 | |
AR054327A1 (es) | Fenil-metanonas sustituidas por heterociclos, procesos de preparacion y composiciones farmaceuticas que lo contienen | |
CA2852609C (en) | Aminopyrimidine derivatives as lrrk2 modulators | |
CO6230984A2 (es) | Inhibidores de cinasa mapk/erk | |
CY1112006T1 (el) | Μακροκυκλικοι αναστολεις του ιου της ηπατιτιδας c | |
AR048055A1 (es) | Derivados de pirimidina como inhibidores de dipeptidil peptidasa | |
EA200971100A1 (ru) | Производные фталазинона в качестве ингибиторов поли(адф-рибоза)полимеразы (parp-1) | |
AR069740A1 (es) | Compuestos nucleosidos antivirales | |
PE20091446A1 (es) | Derivados de isoxazolo-piridazina | |
AR061847A1 (es) | Derivados de pirimidina 2- amino -5- sustituida. como inhibidores de quinasas. composiciones farmaceuticas. | |
RS53176B (en) | KINASE INHIBITORS 1 REGULATING SIGNALS IN APOPTOSIS | |
ATE556058T1 (de) | 1-(2h)-isochinolonderivat | |
ES2613538T3 (es) | Derivados de arilamida como bloqueadores de TTX-S | |
HUP0401784A2 (hu) | Heterobiciklikus szerkezetû virális polimeráz inhibitorok, eljárás az elõállításukra, köztitermékek és ezeket tartalmazó gyógyszerkészítmények | |
AR086590A1 (es) | Compuestos de ciclohexanona y herbicidas que los comprenden | |
CO6150145A2 (es) | Derivados de aril/heterociclo/cicloalquil/cicloalquil fenil substituidos utiles como agentes inmunosupresores | |
NO20076624L (no) | Syklisk aminderivat med substituert alkylgruppe | |
TW200732329A (en) | Aryl-isoxazolo-4-yl-oxadiazole derivatives | |
WO2010005534A3 (en) | Proteasome inhibitors for selectively inducing apoptosis in cancer cells | |
AR061369A1 (es) | Derivados de pirimidina y composiciones farmaceuticas que los comprenden | |
AR082696A1 (es) | Derivados heterociclicos nitrogenados de 1,2,4-oxadiazol, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de enfermedades cardiovasculares e inflamatorias, entre otras | |
EA200800175A1 (ru) | НОВЫЕ ГЕТЕРОЦИКЛИЧЕСКИЕ ИНГИБИТОРЫ NF-κB |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
FB | Suspension of granting procedure |