AR035804A1 - Inhibidores novedosos de tirosina cinasa - Google Patents
Inhibidores novedosos de tirosina cinasaInfo
- Publication number
- AR035804A1 AR035804A1 ARP020101167A ARP020101167A AR035804A1 AR 035804 A1 AR035804 A1 AR 035804A1 AR P020101167 A ARP020101167 A AR P020101167A AR P020101167 A ARP020101167 A AR P020101167A AR 035804 A1 AR035804 A1 AR 035804A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- group
- heteroaryl
- alkenyl
- aryl
- Prior art date
Links
- 102000004022 Protein-Tyrosine Kinases Human genes 0.000 title abstract 3
- 108090000412 Protein-Tyrosine Kinases Proteins 0.000 title abstract 3
- 239000003112 inhibitor Substances 0.000 title 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 4
- 125000001072 heteroaryl group Chemical group 0.000 abstract 4
- 229910052739 hydrogen Inorganic materials 0.000 abstract 4
- 125000003545 alkoxy group Chemical group 0.000 abstract 3
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 125000000304 alkynyl group Chemical group 0.000 abstract 3
- 125000003118 aryl group Chemical group 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 3
- 125000001475 halogen functional group Chemical group 0.000 abstract 3
- 125000004356 hydroxy functional group Chemical group O* 0.000 abstract 3
- 229910052760 oxygen Inorganic materials 0.000 abstract 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 3
- 229910052717 sulfur Inorganic materials 0.000 abstract 3
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 2
- 229910052799 carbon Inorganic materials 0.000 abstract 2
- 201000010099 disease Diseases 0.000 abstract 2
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 2
- 239000001257 hydrogen Substances 0.000 abstract 2
- 125000004435 hydrogen atom Chemical class [H]* 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- 125000005309 thioalkoxy group Chemical group 0.000 abstract 2
- 150000003573 thiols Chemical class 0.000 abstract 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- 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
- 206010003210 Arteriosclerosis Diseases 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 201000004681 Psoriasis Diseases 0.000 abstract 1
- 125000003282 alkyl amino group Chemical group 0.000 abstract 1
- 230000002491 angiogenic effect Effects 0.000 abstract 1
- 208000011775 arteriosclerosis disease Diseases 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 abstract 1
- 206010012601 diabetes mellitus Diseases 0.000 abstract 1
- 125000004663 dialkyl amino group Chemical group 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 239000003937 drug carrier Substances 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 125000004446 heteroarylalkyl group Chemical group 0.000 abstract 1
- 150000004677 hydrates Chemical class 0.000 abstract 1
- 230000002163 immunogen Effects 0.000 abstract 1
- OTXBWGUYZNKPMG-UHFFFAOYSA-N isofulminic acid Chemical compound O[N+]#[C-] OTXBWGUYZNKPMG-UHFFFAOYSA-N 0.000 abstract 1
- 230000002018 overexpression Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 208000037803 restenosis Diseases 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- -1 sulfoxy, sulfonyl Chemical group 0.000 abstract 1
Classifications
-
- 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
- C07D401/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- A61K31/4164—1,3-Diazoles
- A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
-
- 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
-
- 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
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
- C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Un compuesto de conformidad con la fórmula (1), sus enantiómeros, diastereómeros, sales farmacéuticamente aceptables, hidratos, profármacos y solvatos de los mismos; en donde X se selecciona del grupo que consiste de N, C, alquilo C1-3, alquilo C1-3 sustituido con uno o más de R7, y un enlace directo; Y se selecciona del grupo que consiste de O y S; W se selecciona del grupo que consiste de N, C, O, y S, con la condición de que cuando W es O o S, R9 está ausente; R1, R2, R3, R4, R5, R6, R7, R8, R9 cada uno se seleccionan independientemente del grupo que consiste de H, alquilo C1-6, alquenilo, alquinilo, cicloalquilo, heterocicloalquilo, halo, amino, OR60, NO2, OH, SR60, NR60R61, CN, CO2R60, CONR60R61, OCONR60R61, NR62CONR60R61, NR60SO2R61, SO2NR60R61, C(NR62)NR60R61, arilo, heteroarilo, (CH2)nOR60, (CH2)nNR60R61, (CH2)nSR60, (CH2)n arilo, (CH2)nheteroarilo, (CH2)nheterocicloalquilo, NH-Z-arilo, y NH-Z-heteroarilo; en donde n es 1 hasta 3; y Z se selecciona del grupo que consiste de cadena alquilo C1-4, alquenilo, y alquinilo; Z tiene uno o más grupos, hidroxi, tiol, alcoxi, tioalcoxi, amino, halo, NR60SO2R61; Z incorpora opcionalmente uno o más grupos seleccionados del grupo que consiste de CO, CNOH, CNOR60, CNNR60, CNNCOR60 y CNNSO2R60; y R60 y R61 se seleccionan independientemente del grupo que consiste de H, alquilo, alquenilo, alquinilo, cicloalquilo, cicloalquilalquilo, hidroxi, alcoxi, arilo, heteroarilo, heteroarilalquilo y alquilo -R25 en donde R25 es hidrógeno, alquenilo, hidroxi, tiol, alcoxi, tioalcoxi, amino, alquilamino, dialquilamino, arilo, heteroarilo, ciano, halo, sulfoxi, sulfonilo, NR30COOR31, -NR30C(O)R31, -NR30SO2R31, C(O)NR30R31, heteroarilo o heterocicloalquilo; y R30 y R31 son, independientemente, hidrógeno, alquilo, cicloalquilo, o alquilo-R25. Composiciones farmacéuticas que comprenden un compuesto de fórmula (1) y un portador farmacéuticamente aceptable. Los compuestos de fórmula (1) inhiben las enzimas de la tirosina quinasa y son útiles para el tratamiento de enfermedades que se caracterizan por una sobre-expresión o sobre-regulación de la actividad de la tirosina cinasa, tales como cáncer, diabetes, restenosis, arteriosclerosis, psoriasis, enfermedades angiogénicas y desórdenes inmunogénicos.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US27932701P | 2001-03-28 | 2001-03-28 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR035804A1 true AR035804A1 (es) | 2004-07-14 |
Family
ID=23068491
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP020101167A AR035804A1 (es) | 2001-03-28 | 2002-03-27 | Inhibidores novedosos de tirosina cinasa |
Country Status (25)
| Country | Link |
|---|---|
| EP (1) | EP1381598A4 (es) |
| JP (1) | JP2004534010A (es) |
| KR (1) | KR20030083016A (es) |
| CN (1) | CN1514833A (es) |
| AR (1) | AR035804A1 (es) |
| BG (1) | BG108206A (es) |
| BR (1) | BR0208373A (es) |
| CA (1) | CA2442428A1 (es) |
| CZ (1) | CZ20032615A3 (es) |
| EE (1) | EE200300475A (es) |
| GE (1) | GEP20053660B (es) |
| HR (1) | HRP20030844A2 (es) |
| HU (1) | HUP0400323A2 (es) |
| IL (1) | IL158041A0 (es) |
| IS (1) | IS6968A (es) |
| MX (1) | MXPA03008690A (es) |
| NO (1) | NO20034308L (es) |
| PE (1) | PE20021015A1 (es) |
| PL (1) | PL373300A1 (es) |
| RU (1) | RU2003131693A (es) |
| SK (1) | SK12002003A3 (es) |
| UY (1) | UY27234A1 (es) |
| WO (1) | WO2002079192A1 (es) |
| YU (1) | YU84603A (es) |
| ZA (1) | ZA200307466B (es) |
Families Citing this family (59)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7081454B2 (en) * | 2001-03-28 | 2006-07-25 | Bristol-Myers Squibb Co. | Tyrosine kinase inhibitors |
| AU2003218236B2 (en) | 2002-03-01 | 2007-12-06 | Bristol-Myers Squibb Company | Transgenic non-human mammals expressing constitutively activated tyrosine kinase receptors |
| AU2003243497A1 (en) * | 2002-06-12 | 2003-12-31 | Millennium Pharmaceuticals, Inc. | Antagonists of melanin concentrating hormone receptor |
| WO2004050033A2 (en) * | 2002-12-02 | 2004-06-17 | Arqule, Inc. | Method of treating cancers |
| EP1581539A4 (en) | 2003-01-03 | 2007-09-19 | Bristol Myers Squibb Co | NEW TYROSINE KINASE HEMMER |
| JP2006516626A (ja) * | 2003-01-28 | 2006-07-06 | スミスクライン ビーチャム コーポレーション | 化学的化合物 |
| US7312215B2 (en) | 2003-07-29 | 2007-12-25 | Bristol-Myers Squibb Company | Benzimidazole C-2 heterocycles as kinase inhibitors |
| CA2536954C (en) | 2003-08-29 | 2012-11-27 | Exelixis, Inc. | C-kit modulators and methods of use |
| US20050075358A1 (en) * | 2003-10-06 | 2005-04-07 | Carboni Joan M. | Methods for treating IGF1R-inhibitor induced hyperglycemia |
| US7572914B2 (en) | 2003-12-19 | 2009-08-11 | Takeda Pharmaceutical Company Limited | Kinase inhibitors |
| DE102004010207A1 (de) | 2004-03-02 | 2005-09-15 | Aventis Pharma S.A. | Neue 4-Benzimidazol-2-yl-pyridazin-3-on-Derivate |
| EP2305682A1 (en) | 2004-04-02 | 2011-04-06 | OSI Pharmaceuticals, Inc. | 6,6-bicyclic ring substituted heterobicyclic protein kinase inhibitors |
| US7550598B2 (en) | 2004-08-18 | 2009-06-23 | Takeda Pharmaceutical Company Limited | Kinase inhibitors |
| JP2008524233A (ja) * | 2004-12-16 | 2008-07-10 | 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 | 炎症性疾患、増殖性疾患および免疫介在性疾患の治療のためのｔｅｃファミリータンパク質キナーゼのインヒビターとして有用なピリド−２−オン |
| US7582634B2 (en) | 2005-02-18 | 2009-09-01 | Wyeth | 7-substituted imidazo[4,5-c]pyridine antagonists of gonadotropin releasing hormone receptor |
| US7538113B2 (en) | 2005-02-18 | 2009-05-26 | Wyeth | 4-substituted imidazo[4,5-c]pyridine antagonists of gonadotropin releasing hormone receptor |
| US7534796B2 (en) | 2005-02-18 | 2009-05-19 | Wyeth | Imidazo[4,5-b]pyridine antagonists of gonadotropin releasing hormone receptor |
| US7531542B2 (en) | 2005-05-18 | 2009-05-12 | Wyeth | Benzooxazole and benzothiazole antagonists of gonadotropin releasing hormone receptor |
| US7582636B2 (en) | 2005-05-26 | 2009-09-01 | Wyeth | Piperazinylimidazopyridine and piperazinyltriazolopyridine antagonists of Gonadotropin Releasing Hormone receptor |
| WO2006130657A2 (en) | 2005-05-31 | 2006-12-07 | Bristol-Myers Squibb Company | Stereoselective reduction process for the preparation of pyrrolotriazine compounds |
| US8088928B2 (en) | 2005-08-04 | 2012-01-03 | Sirtris Pharmaceuticals, Inc. | Sirtuin modulating compounds |
| US7855289B2 (en) | 2005-08-04 | 2010-12-21 | Sirtris Pharmaceuticals, Inc. | Sirtuin modulating compounds |
| EP2468752A1 (en) | 2005-08-04 | 2012-06-27 | Sirtris Pharmaceuticals, Inc. | Thiazolopyridine derivatives as sirtuin-modulators |
| US8093401B2 (en) | 2005-08-04 | 2012-01-10 | Sirtris Pharmaceuticals, Inc. | Sirtuin modulating compounds |
| DE602006020293D1 (de) | 2005-08-29 | 2011-04-07 | Vertex Pharma | 3,5-disubstituierte pyrid-2-one, die als hemmer der tec-familie von nicht-rezeptor tyrosin-kinasen nützlich sind |
| EP1919906B1 (en) | 2005-08-29 | 2011-10-12 | Vertex Pharmaceuticals Incorporated | 3, 5-disubstituted pyrid-2-ones useful as inhibitors of tec family of non-receptor tyrosine kinases |
| AU2006285038A1 (en) | 2005-08-29 | 2007-03-08 | Vertex Pharmaceuticals Incorporated | 3,5-disubstituted pyrid-2-ones useful as inhibitors of Tec family of non-receptor tyrosine kinases |
| WO2007026720A1 (ja) * | 2005-08-31 | 2007-03-08 | Taisho Pharmaceutical Co., Ltd. | 縮環ピラゾール誘導体 |
| US8575164B2 (en) | 2005-12-19 | 2013-11-05 | OSI Pharmaceuticals, LLC | Combination cancer therapy |
| WO2007145203A1 (ja) * | 2006-06-13 | 2007-12-21 | Daiichi Fine Chemical Co., Ltd. | 光学活性２－アミノ－１－（４－フルオロフェニル）エタノール |
| US8063225B2 (en) * | 2006-08-14 | 2011-11-22 | Chembridge Corporation | Tricyclic compound derivatives useful in the treatment of neoplastic diseases, inflammatory disorders and immunomodulatory disorders |
| WO2008022747A1 (en) * | 2006-08-21 | 2008-02-28 | F. Hoffmann-La Roche Ag | Tricyclic lactam derivatives, their manufacture and use as pharmaceutical agents |
| WO2008025526A1 (en) * | 2006-08-31 | 2008-03-06 | F. Hoffmann-La Roche Ag | Indole derivatives, their manufacture and use as pharmaceutical agents |
| US8492328B2 (en) | 2007-05-17 | 2013-07-23 | Bristol-Myers Squibb Company | Biomarkers and methods for determining sensitivity to insulin growth factor-1 receptor modulators |
| CL2008001822A1 (es) | 2007-06-20 | 2009-03-13 | Sirtris Pharmaceuticals Inc | Compuestos derivados de tiazolo[5,4-b]piridina; composicion farmaceutica que comprende a dichos compuestos; y uso del compuesto en el tratamiento de la resistencia a la insulina, sindrome metabolico, diabetes, entre otras. |
| WO2009000489A1 (en) * | 2007-06-25 | 2008-12-31 | F. Hoffmann-La Roche Ag | Benzimidazole amido derivatives as kinase inhibitors |
| EP2065380A1 (en) * | 2007-08-22 | 2009-06-03 | F.Hoffmann-La Roche Ag | Pyridoneamide derivatives as focal adhesion kinase (FAK) inhibitors and their use for the treatment of cancer |
| US7816540B2 (en) * | 2007-12-21 | 2010-10-19 | Hoffmann-La Roche Inc. | Carboxyl- or hydroxyl-substituted benzimidazole derivatives |
| WO2009093012A1 (en) | 2008-01-22 | 2009-07-30 | Vernalis (R & D) Ltd | Indolyl- pyridone derivatives having checkpoint kinase 1 inhibitory activity |
| EP2283020B8 (en) | 2008-05-19 | 2012-12-12 | OSI Pharmaceuticals, LLC | Substituted imidazopyr-and imidazotri-azines |
| UA104447C2 (uk) | 2008-12-19 | 2014-02-10 | Сіртріз Фармасьютікалз, Інк. | Тіазолопіридинові сполуки, що модулюють сиртуїн |
| DE102010001064A1 (de) * | 2009-03-18 | 2010-09-23 | Bayer Schering Pharma Aktiengesellschaft | Substituierte 2-Acetamido-5-Aryl-1,2,4-triazolone und deren Verwendung |
| EP2421837A1 (en) | 2009-04-20 | 2012-02-29 | OSI Pharmaceuticals, LLC | Preparation of c-pyrazine-methylamines |
| WO2010138575A1 (en) * | 2009-05-27 | 2010-12-02 | Abbott Laboratories | Pyrimidine inhibitors of kinase activity |
| US20120220594A1 (en) | 2009-10-30 | 2012-08-30 | Bristol-Meyers Squibb Company | Methods for treating cancer in patients having igf-1r inhibitor resistance |
| CN103124496B (zh) * | 2010-10-06 | 2016-03-30 | 葛兰素史密丝克莱恩有限责任公司 | 作为pi3激酶抑制剂的苯并咪唑衍生物 |
| US8772304B2 (en) * | 2010-11-01 | 2014-07-08 | Boehringer Ingelheim International Gmbh | Benzimidazole inhibitors of leukotriene production |
| WO2013056069A1 (en) | 2011-10-13 | 2013-04-18 | Bristol-Myers Squibb Company | Methods for selecting and treating cancer in patients with igf-1r/ir inhibitors |
| JP6461121B2 (ja) | 2013-06-21 | 2019-01-30 | ゼニス・エピジェネティクス・リミテッドＺｅｎｉｔｈ Ｅｐｉｇｅｎｅｔｉｃｓ Ｌｔｄ． | 新規の二環式ブロモドメイン阻害剤 |
| WO2015004534A2 (en) | 2013-06-21 | 2015-01-15 | Zenith Epigenetics Corp. | Novel substituted bicyclic compounds as bromodomain inhibitors |
| CN105593224B (zh) | 2013-07-31 | 2021-05-25 | 恒元生物医药科技(苏州)有限公司 | 作为溴结构域抑制剂的新型喹唑啉酮类化合物 |
| CN103936719A (zh) * | 2014-05-14 | 2014-07-23 | 中国药科大学 | 苯并咪唑类衍生物制备方法及用途 |
| EP3194572B1 (en) | 2014-07-30 | 2023-10-25 | Yeda Research and Development Co. Ltd. | Media for culturing pluripotent stem cells |
| US10710992B2 (en) | 2014-12-01 | 2020-07-14 | Zenith Epigenetics Ltd. | Substituted pyridinones as bromodomain inhibitors |
| US10292968B2 (en) | 2014-12-11 | 2019-05-21 | Zenith Epigenetics Ltd. | Substituted heterocycles as bromodomain inhibitors |
| CN107406438B (zh) | 2014-12-17 | 2021-05-14 | 恒翼生物医药科技(上海)有限公司 | 溴结构域的抑制剂 |
| EP3283475B1 (en) * | 2015-04-16 | 2019-10-16 | Merck Patent GmbH | 3-(1h-benzimidazol-2-yl)-1h-pyridin-2-one derivatives |
| WO2020152686A1 (en) | 2019-01-23 | 2020-07-30 | Yeda Research And Development Co. Ltd. | Culture media for pluripotent stem cells |
| CN117069696B (zh) * | 2023-08-17 | 2024-04-26 | 中国药科大学 | 一种双靶点小分子抑制剂及其制备方法和应用 |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6162804A (en) * | 1997-09-26 | 2000-12-19 | Merck & Co., Inc. | Tyrosine kinase inhibitors |
| ME00370B (me) * | 1999-06-23 | 2011-05-10 | Sanofi Aventis Deutschland | SUPSTITUISANI BENZIMIDAZOLl |
| US7081454B2 (en) * | 2001-03-28 | 2006-07-25 | Bristol-Myers Squibb Co. | Tyrosine kinase inhibitors |
-
2002
- 2002-03-26 SK SK12002003A patent/SK12002003A3/sk not_active Application Discontinuation
- 2002-03-26 CZ CZ20032615A patent/CZ20032615A3/cs unknown
- 2002-03-26 RU RU2003131693/04A patent/RU2003131693A/ru not_active Application Discontinuation
- 2002-03-26 CA CA002442428A patent/CA2442428A1/en not_active Abandoned
- 2002-03-26 CN CNA028105168A patent/CN1514833A/zh active Pending
- 2002-03-26 WO PCT/US2002/009402 patent/WO2002079192A1/en not_active Ceased
- 2002-03-26 HU HU0400323A patent/HUP0400323A2/hu unknown
- 2002-03-26 JP JP2002577817A patent/JP2004534010A/ja not_active Withdrawn
- 2002-03-26 BR BR0208373-6A patent/BR0208373A/pt not_active IP Right Cessation
- 2002-03-26 EP EP02723631A patent/EP1381598A4/en not_active Withdrawn
- 2002-03-26 MX MXPA03008690A patent/MXPA03008690A/es unknown
- 2002-03-26 EE EEP200300475A patent/EE200300475A/xx unknown
- 2002-03-26 PL PL02373300A patent/PL373300A1/xx not_active Application Discontinuation
- 2002-03-26 KR KR10-2003-7012594A patent/KR20030083016A/ko not_active Withdrawn
- 2002-03-26 YU YU84603A patent/YU84603A/sh unknown
- 2002-03-26 IL IL15804102A patent/IL158041A0/xx unknown
- 2002-03-26 GE GE5363A patent/GEP20053660B/en unknown
- 2002-03-26 HR HR20030844A patent/HRP20030844A2/hr not_active Application Discontinuation
- 2002-03-27 UY UY27234A patent/UY27234A1/es not_active Application Discontinuation
- 2002-03-27 AR ARP020101167A patent/AR035804A1/es not_active Application Discontinuation
- 2002-03-27 PE PE2002000244A patent/PE20021015A1/es not_active Application Discontinuation
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2003
- 2003-09-25 ZA ZA200307466A patent/ZA200307466B/en unknown
- 2003-09-26 IS IS6968A patent/IS6968A/is unknown
- 2003-09-26 BG BG108206A patent/BG108206A/bg unknown
- 2003-09-26 NO NO20034308A patent/NO20034308L/no not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| KR20030083016A (ko) | 2003-10-23 |
| WO2002079192A1 (en) | 2002-10-10 |
| EP1381598A1 (en) | 2004-01-21 |
| PE20021015A1 (es) | 2002-11-10 |
| CZ20032615A3 (en) | 2004-03-17 |
| BR0208373A (pt) | 2005-02-22 |
| HUP0400323A2 (hu) | 2005-11-28 |
| JP2004534010A (ja) | 2004-11-11 |
| UY27234A1 (es) | 2002-10-31 |
| NO20034308L (no) | 2003-11-26 |
| EP1381598A4 (en) | 2008-03-19 |
| PL373300A1 (en) | 2005-08-22 |
| CA2442428A1 (en) | 2002-10-10 |
| BG108206A (bg) | 2004-11-30 |
| HRP20030844A2 (en) | 2005-08-31 |
| MXPA03008690A (es) | 2003-12-12 |
| IL158041A0 (en) | 2004-03-28 |
| RU2003131693A (ru) | 2005-05-10 |
| YU84603A (sh) | 2006-03-03 |
| EE200300475A (et) | 2004-02-16 |
| SK12002003A3 (en) | 2004-10-05 |
| IS6968A (is) | 2003-09-26 |
| GEP20053660B (en) | 2005-11-10 |
| CN1514833A (zh) | 2004-07-21 |
| NO20034308D0 (no) | 2003-09-26 |
| ZA200307466B (en) | 2005-01-13 |
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