HRP20120351T1 - Macrociklički derivati kinazolina kao antiproliferativna sredstva - Google Patents
Macrociklički derivati kinazolina kao antiproliferativna sredstva Download PDFInfo
- Publication number
- HRP20120351T1 HRP20120351T1 HRP20120351TT HRP20120351T HRP20120351T1 HR P20120351 T1 HRP20120351 T1 HR P20120351T1 HR P20120351T T HRP20120351T T HR P20120351TT HR P20120351 T HRP20120351 T HR P20120351T HR P20120351 T1 HRP20120351 T1 HR P20120351T1
- Authority
- HR
- Croatia
- Prior art keywords
- 4alkyl
- hydroxy
- optionally substituted
- alkyl
- amino
- Prior art date
Links
- 230000001028 anti-proliverative effect Effects 0.000 title 1
- 125000002294 quinazolinyl group Chemical class N1=C(N=CC2=CC=CC=C12)* 0.000 title 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims abstract 107
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims abstract 46
- 150000001875 compounds Chemical class 0.000 claims abstract 22
- 150000003839 salts Chemical class 0.000 claims abstract 5
- 125000000815 N-oxide group Chemical group 0.000 claims abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 98
- 239000001257 hydrogen Substances 0.000 claims 98
- -1 hydroxy, formyl Chemical group 0.000 claims 96
- 125000001424 substituent group Chemical group 0.000 claims 94
- 125000000623 heterocyclic group Chemical group 0.000 claims 71
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 66
- 125000000217 alkyl group Chemical group 0.000 claims 65
- 125000003386 piperidinyl group Chemical group 0.000 claims 65
- 150000002431 hydrogen Chemical class 0.000 claims 59
- 125000001475 halogen functional group Chemical group 0.000 claims 54
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 51
- 125000004193 piperazinyl group Chemical group 0.000 claims 50
- 125000002757 morpholinyl group Chemical group 0.000 claims 47
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 40
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 37
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 37
- 125000004093 cyano group Chemical group *C#N 0.000 claims 20
- 125000002883 imidazolyl group Chemical group 0.000 claims 19
- 125000003545 alkoxy group Chemical group 0.000 claims 14
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 13
- 125000000335 thiazolyl group Chemical group 0.000 claims 13
- 125000005879 dioxolanyl group Chemical group 0.000 claims 11
- 125000002541 furyl group Chemical group 0.000 claims 11
- 125000001041 indolyl group Chemical group 0.000 claims 11
- 125000000842 isoxazolyl group Chemical group 0.000 claims 11
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 11
- 125000002971 oxazolyl group Chemical group 0.000 claims 11
- 125000003226 pyrazolyl group Chemical group 0.000 claims 11
- 125000004076 pyridyl group Chemical group 0.000 claims 11
- ORTFAQDWJHRMNX-UHFFFAOYSA-N hydroxidooxidocarbon(.) Chemical group O[C]=O ORTFAQDWJHRMNX-UHFFFAOYSA-N 0.000 claims 10
- 239000000543 intermediate Substances 0.000 claims 9
- QMMFVYPAHWMCMS-UHFFFAOYSA-N Dimethyl sulfide Chemical group CSC QMMFVYPAHWMCMS-UHFFFAOYSA-N 0.000 claims 8
- ROSDSFDQCJNGOL-UHFFFAOYSA-N Dimethylamine Chemical group CNC ROSDSFDQCJNGOL-UHFFFAOYSA-N 0.000 claims 8
- 150000001412 amines Chemical group 0.000 claims 8
- 125000002795 guanidino group Chemical group C(N)(=N)N* 0.000 claims 8
- 125000004464 hydroxyphenyl group Chemical group 0.000 claims 8
- 150000003573 thiols Chemical group 0.000 claims 8
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 7
- 125000004769 (C1-C4) alkylsulfonyl group Chemical group 0.000 claims 6
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims 6
- 125000005883 dithianyl group Chemical group 0.000 claims 6
- 125000004568 thiomorpholinyl group Chemical group 0.000 claims 6
- 125000004760 (C1-C4) alkylsulfonylamino group Chemical group 0.000 claims 5
- NCWDBNBNYVVARF-UHFFFAOYSA-N 1,3,2-dioxaborolane Chemical compound B1OCCO1 NCWDBNBNYVVARF-UHFFFAOYSA-N 0.000 claims 5
- ZADPBFCGQRWHPN-UHFFFAOYSA-N boronic acid Chemical compound OBO ZADPBFCGQRWHPN-UHFFFAOYSA-N 0.000 claims 5
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 claims 5
- 230000015572 biosynthetic process Effects 0.000 claims 4
- MHZKZYGZVUKOGK-UHFFFAOYSA-N 16-oxa-2,10,21,23-tetrazatetracyclo[15.6.2.03,8.020,24]pentacosa-1(23),2,4,6,8,10,12,14,17(25),18,20(24),21-dodecaene Chemical compound O1C=CC=CC=NC=C2C=CC=CC2=NC2=NC=NC3=CC=C1C=C23 MHZKZYGZVUKOGK-UHFFFAOYSA-N 0.000 claims 3
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 3
- 101100070530 Neurospora crassa (strain ATCC 24698 / 74-OR23-1A / CBS 708.71 / DSM 1257 / FGSC 987) het-6 gene Proteins 0.000 claims 3
- 238000010511 deprotection reaction Methods 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 238000003786 synthesis reaction Methods 0.000 claims 3
- ZZYURNCXESTFFO-UHFFFAOYSA-N 18-oxa-2,10,13,23,25-pentazatetracyclo[17.6.2.03,8.022,26]heptacosa-1(25),2,4,6,8,10,13,15,19(27),20,22(26),23-dodecaen-12-one Chemical compound O1CC=CC=NC(=O)C=NC=C2C=CC=CC2=NC2=NC=NC3=CC=C1C=C23 ZZYURNCXESTFFO-UHFFFAOYSA-N 0.000 claims 2
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 125000004674 methylcarbonyl group Chemical group CC(=O)* 0.000 claims 2
- 125000006239 protecting group Chemical group 0.000 claims 2
- 238000006798 ring closing metathesis reaction Methods 0.000 claims 2
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 2
- 125000004665 trialkylsilyl group Chemical group 0.000 claims 2
- 125000006527 (C1-C5) alkyl group Chemical group 0.000 claims 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 1
- BBLPPTZXJGLEMM-UHFFFAOYSA-N 16-oxa-2,10,13,21,23-pentazatetracyclo[15.6.2.03,8.020,24]pentacosa-1(23),2,4,6,8,10,12,14,17(25),18,20(24),21-dodecaene Chemical compound O1C=CN=CC=NC=C2C=CC=CC2=NC2=NC=NC3=CC=C1C=C23 BBLPPTZXJGLEMM-UHFFFAOYSA-N 0.000 claims 1
- ZAZXJWBRSZKYBG-UHFFFAOYSA-N 18-oxa-2,10,13,23,25-pentazatetracyclo[17.6.2.03,8.022,26]heptacosa-1(25),2,4,6,8,10,12,14,16,19(27),20,22(26),23-tridecaene Chemical compound O1C=CC=CN=CC=NC=C2C=CC=CC2=NC2=NC=NC3=CC=C1C=C23 ZAZXJWBRSZKYBG-UHFFFAOYSA-N 0.000 claims 1
- MXMLDVCCERTVHX-UHFFFAOYSA-N 20-oxa-2,10,16,25,27-pentazapentacyclo[19.6.2.110,14.03,8.024,28]triaconta-1(27),2,4,6,8,11,13,16,18,21(29),22,24(28),25-tridecaen-15-one Chemical compound N1=CN=C2N=C3C=CC=CC3=CN(C=CC=3)CC=3C(=O)N=CC=COC3=CC=C1C2=C3 MXMLDVCCERTVHX-UHFFFAOYSA-N 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 108091000080 Phosphotransferase Proteins 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 150000001298 alcohols Chemical class 0.000 claims 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 1
- 150000001448 anilines Chemical class 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 230000008878 coupling Effects 0.000 claims 1
- 238000010168 coupling process Methods 0.000 claims 1
- 238000005859 coupling reaction Methods 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 229940043355 kinase inhibitor Drugs 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 102000020233 phosphotransferase Human genes 0.000 claims 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 claims 1
- 230000002062 proliferating effect Effects 0.000 claims 1
- YSKSQFPXRWBHAZ-UHFFFAOYSA-N quinazolin-6-yl acetate Chemical compound N1=CN=CC2=CC(OC(=O)C)=CC=C21 YSKSQFPXRWBHAZ-UHFFFAOYSA-N 0.000 claims 1
- 239000011347 resin Substances 0.000 claims 1
- 229920005989 resin Polymers 0.000 claims 1
- 208000037803 restenosis Diseases 0.000 claims 1
- 239000007790 solid phase Substances 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/06—Peri-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- 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
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
- C07C229/02—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
- C07C229/04—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
- C07C229/06—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton
- C07C229/10—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings
- C07C229/16—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings to carbon atoms of hydrocarbon radicals substituted by amino or carboxyl groups, e.g. ethylenediamine-tetra-acetic acid, iminodiacetic acids
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
- C07C229/40—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino groups bound to carbon atoms of at least one six-membered aromatic ring and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
- C07D239/88—Oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
- C07D239/93—Sulfur atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
- C07D239/94—Nitrogen atoms
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP0305723 | 2003-05-27 | ||
| EP0310266 | 2003-09-15 | ||
| EP0351061 | 2003-12-18 | ||
| PCT/EP2004/005621 WO2004105765A1 (en) | 2003-05-27 | 2004-05-25 | Macrocyclic quinazoline derivatives as antiproliferative agents |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20120351T1 true HRP20120351T1 (hr) | 2012-05-31 |
Family
ID=33493782
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20120351TT HRP20120351T1 (hr) | 2003-05-27 | 2012-04-19 | Macrociklički derivati kinazolina kao antiproliferativna sredstva |
Country Status (32)
| Country | Link |
|---|---|
| US (4) | US7648975B2 (es) |
| EP (2) | EP1633365B1 (es) |
| JP (1) | JP4887151B2 (es) |
| KR (1) | KR101143878B1 (es) |
| CN (1) | CN102718775B (es) |
| AR (2) | AR045687A1 (es) |
| AT (1) | ATE544454T1 (es) |
| AU (1) | AU2004243487B2 (es) |
| BR (1) | BRPI0410714B8 (es) |
| CA (1) | CA2525214C (es) |
| CL (1) | CL2004001267A1 (es) |
| CO (1) | CO5640038A2 (es) |
| CY (1) | CY1113002T1 (es) |
| DK (1) | DK1633365T3 (es) |
| EA (1) | EA009064B1 (es) |
| ES (1) | ES2381976T3 (es) |
| HK (1) | HK1176350A1 (es) |
| HR (1) | HRP20120351T1 (es) |
| IL (3) | IL172154A0 (es) |
| IS (1) | IS3030B (es) |
| JO (1) | JO2785B1 (es) |
| MX (1) | MXPA05012762A (es) |
| MY (1) | MY148633A (es) |
| NO (1) | NO334209B1 (es) |
| NZ (1) | NZ544154A (es) |
| PA (1) | PA8603801A1 (es) |
| PL (1) | PL1633365T3 (es) |
| PT (1) | PT1633365E (es) |
| SI (1) | SI1633365T1 (es) |
| TW (3) | TWI468397B (es) |
| UA (1) | UA84010C2 (es) |
| WO (1) | WO2004105765A1 (es) |
Families Citing this family (51)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JO2785B1 (en) * | 2003-05-27 | 2014-03-15 | شركة جانسين فارماسوتيكا ان. في | Quinazoline derivatives |
| EP1684762A4 (en) * | 2003-11-13 | 2009-06-17 | Ambit Biosciences Corp | UREA DERIVATIVES AS MODULATORS OF KINASE |
| US7799772B2 (en) * | 2003-12-18 | 2010-09-21 | Janssen Pharmaceutica N.V. | Pyrido-and pyrimidopyrimidine derivatives as anti-profilerative agents |
| EP1696914B1 (en) * | 2003-12-18 | 2009-10-28 | Janssen Pharmaceutica N.V. | 3-cyano-quinoline derivatives with antiproliferative activity |
| NI200700147A (es) | 2004-12-08 | 2019-05-10 | Janssen Pharmaceutica Nv | Derivados de quinazolina inhibidores de cinasas dirigidos a multip |
| MY169441A (en) | 2004-12-08 | 2019-04-11 | Janssen Pharmaceutica Nv | 2,4, (4,6) pyrimidine derivatives |
| JO3088B1 (ar) * | 2004-12-08 | 2017-03-15 | Janssen Pharmaceutica Nv | مشتقات كوينازولين كبيرة الحلقات و استعمالها بصفتها موانع كينيز متعددة الاهداف |
| CA2599328C (en) | 2005-02-23 | 2012-04-17 | Shionogi & Co., Ltd. | Quinazoline derivative having tyrosine kinase inhibitory activity |
| GB0509227D0 (en) * | 2005-05-05 | 2005-06-15 | Chroma Therapeutics Ltd | Intracellular enzyme inhibitors |
| JP5345388B2 (ja) * | 2005-06-30 | 2013-11-20 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | 環式アニリノ−ピリジノトリアジン |
| JP2009542778A (ja) * | 2006-07-13 | 2009-12-03 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | Ｍｔｋｉキナゾリン誘導体 |
| JP2009242240A (ja) * | 2006-08-04 | 2009-10-22 | Mebiopharm Co Ltd | 含ホウ素キナゾリン誘導体 |
| WO2008033748A2 (en) * | 2006-09-11 | 2008-03-20 | Curis, Inc. | Quinazoline based egfr inhibitors containing a zinc binding moiety |
| BRPI0715016A2 (pt) | 2006-09-11 | 2013-05-28 | Curis Inc | composiÇço, composiÇço farmacÊutica, mÉtodo para tratar uma doenÇa ou distérbio relacionada com tirosina quinase de egfr em um individuo necessitando o mesmo, mÉtodo para tratar uma doenÇa mediada por hdac e mÉtodo para tratar doenÇas medidas tanto por tirosina quinase de egfr quanto hdac |
| US7547781B2 (en) | 2006-09-11 | 2009-06-16 | Curis, Inc. | Quinazoline based EGFR inhibitors containing a zinc binding moiety |
| EP2101782A2 (en) * | 2006-10-27 | 2009-09-23 | Janssen Pharmaceutica N.V. | Use of mtki 1 for treating or preventing bone cancer |
| EP2407783A1 (en) * | 2006-10-27 | 2012-01-18 | Janssen Pharmaceutica, N.V. | A method for pharmacologically profiling compounds |
| EP2077845A2 (en) * | 2006-10-27 | 2009-07-15 | Janssen Pharmaceutica N.V. | Macrocyclic quinazoline derivatives as vegfr3 inhibitors |
| CA2664145A1 (en) * | 2006-10-27 | 2008-05-02 | Janssen Pharmaceutica Nv | Use of a mt kinase inhibitor for treating or preventing brain cancer |
| JPWO2008087736A1 (ja) * | 2007-01-19 | 2010-05-06 | 宇部興産株式会社 | アラルキルオキシ又はヘテロアラルキルオキシ基を有する芳香族アミンの製法 |
| US8642067B2 (en) | 2007-04-02 | 2014-02-04 | Allergen, Inc. | Methods and compositions for intraocular administration to treat ocular conditions |
| JP5536647B2 (ja) | 2007-07-27 | 2014-07-02 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | ピロロピリミジン |
| US8119616B2 (en) | 2007-09-10 | 2012-02-21 | Curis, Inc. | Formulation of quinazoline based EGFR inhibitors containing a zinc binding moiety |
| CL2008003384A1 (es) * | 2007-11-14 | 2009-12-11 | Enanta Pharm Inc | Compuestos derivados de quinoxalina macrocíclica, inhibidores de serina proteasa; composicion farmaceutica que los comprende; y su uso en el tratamiento de la hepatitis c. |
| US8426430B2 (en) | 2008-06-30 | 2013-04-23 | Hutchison Medipharma Enterprises Limited | Quinazoline derivatives |
| EP2350075B1 (en) | 2008-09-22 | 2014-03-05 | Array Biopharma, Inc. | Substituted imidazo[1,2b]pyridazine compounds as trk kinase inhibitors |
| HUE057625T2 (hu) | 2008-10-22 | 2022-05-28 | Array Biopharma Inc | TRK kináz inhibitor szubsztituált pirazolo[1,5-a]pirimidin vegyületek |
| WO2010085597A1 (en) * | 2009-01-23 | 2010-07-29 | Incyte Corporation | Macrocyclic compounds and their use as kinase inhibitors |
| AR077468A1 (es) | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
| TWI406853B (zh) * | 2010-04-07 | 2013-09-01 | Dev Center Biotechnology | Ｅｇｆｒ與ｖｅｇｆｒ－２雙重抑制劑及其用途與製法 |
| WO2011146336A1 (en) * | 2010-05-20 | 2011-11-24 | Array Biopharma Inc. | Macrocyclic compounds as trk kinase inhibitors |
| WO2013126015A1 (en) | 2012-02-23 | 2013-08-29 | N. V. Nutricia | Composition comprising non- digestible oligosaccharides |
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| BE558251A (es) * | 1956-06-11 | |||
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| EP0892789B2 (en) * | 1996-04-12 | 2009-11-18 | Warner-Lambert Company LLC | Irreversible inhibitors of tyrosine kinases |
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